DGIdb - DASATINIB Drug Record

DASATINIB chembl:CHEMBL1421 ApprovedAntineoplasticImmunotherapy

Alternate Names:

SPRYCEL
DASATINIB
BMS-354825 HYDRATE
BMS-354825
DASATINIB HYDRATE
BMS-354825-03
DASATINIB MONOHYDRATE
BMS 345825
BMS 35482513
ANHYDROUS DASATINIB
BMS 354825
SPRYCEL®
ANH. DASATINIB
DASATINIB ANHYDROUS
DASATINIB (ANH.)
chemidplus:302962-49-8
drugbank:01254
pubchem.compound:3062316
chembl:CHEMBL1421
rxcui:1546019

Drug Info:

Year of Approval	2006
Drug Class	antineoplastic agents, protein kinase inhibitors
FDA Approval	Chronic myelogenous leukemia (Philadelphia chromosome positive), Acute lymphoblastic leukemia (Ph +)
Drug Class	Kinase Inhibitors
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Source Reported Drug Name(s)	Dasatinib/Sprycel/ BMS-354825
Pharmaceutical Developer	Bristol-Myers Squibb
Source Reported Drug Name(s)	Dasatinib
Drug Class	Kit Inhibitor

(15 More Sources)

Publications:

Faoro et al., 2010, EphA2 mutation in lung squamous cell carcinoma promotes increased cell survival, cell invasion, focal adhesions, and mammalian target of rapamycin activation., J. Biol. Chem.
Lindauer et al., 2010, Dasatinib., Recent Results Cancer Res.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer
Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.
Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
Tomita O et al., 2014, Sensitivity of SNX2-ABL1 toward tyrosine kinase inhibitors distinct from that of BCR-ABL1., Leuk Res
Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med
Jabbour et al., 2008, Characteristics and outcome of chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors., Blood
Burgess MR et al., 2005, Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance., Proc Natl Acad Sci U S A
Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature
Bradeen HA et al., 2006, Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations., Blood
Müller MC et al., 2009, Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations., Blood
Talpaz M et al., 2006, Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias., N Engl J Med
An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
Strhakova et al., 2011, Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia., Neoplasma
Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
Sorel et al., 2004, Evidence of ABL-kinase domain mutations in highly purified primitive stem cell populations of patients with chronic myelogenous leukemia., Biochem. Biophys. Res. Commun.
Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
Doi et al., 2009, High-resolution melting analysis for a reliable and two-step scanning of mutations in the tyrosine kinase domain of the chimerical bcr-abl gene., Int. J. Hematol.
O'Hare et al., 2004, Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML., Blood
Elias et al., 2014, BCR-ABL kinase domain mutations, including 2 novel mutations in imatinib resistant Malaysian chronic myeloid leukemia patients-Frequency and clinical outcome., Leuk. Res.
Qin et al., 2011, Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients., Ann. Hematol.
Hughes et al., 2009, Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase., J. Clin. Oncol.
Al-Ali et al., 2004, High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib., Hematol. J.
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Jones et al., 2008, Kinase domain point mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia emerge after therapy with BCR-ABL kinase inhibitors., Cancer
von Bubnoff et al., 2003, Inhibition of wild-type and mutant Bcr-Abl by pyrido-pyrimidine-type small molecule kinase inhibitors., Cancer Res.
von Bubnoff et al., 2002, BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study., Lancet
Branford et al., 2002, High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance., Blood
Eide et al., 2011, The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile., Cancer Res.
Hochhaus et al., 2002, Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy., Leukemia
Soverini et al., 2011, BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet., Blood
Piccaluga et al., 2007, Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia., Cancer
Deguchi Y et al., 2008, Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines., Leuk Res
Pitini et al., 2013, Response to dasatinib in a patient with SQCC of the lung harboring a discoid-receptor-2 and synchronous chronic myelogenous leukemia., Lung Cancer
Day et al., 2008, Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib., Eur. J. Pharmacol.
Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
Koschmann C et al., 2016, Characterizing and targeting PDGFRA alterations in pediatric high-grade glioma., Oncotarget
Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
Rizzo et al., 2010, Prognostic vs predictive molecular biomarkers in colorectal cancer: is KRAS and BRAF wild type status required for anti-EGFR therapy?, Cancer Treat. Rev.
Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
Nam et al., 2005, Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells., Cancer Res.
Kamath et al., 2008, Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL., Cancer Chemother. Pharmacol.
Quintás-Cardama et al., 2006, Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib., Future Oncol
Schittenhelm et al., 2006, Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies., Cancer Res.
Serrels et al., 2006, Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib., Mol. Cancer Ther.
Getlik M et al., 2009, Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc., J Med Chem
Zhang CH et al., 2015, Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer., J Med Chem
Du et al., 2009, Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy., Nat. Biotechnol.
Saha et al., 2016, Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma., Cancer Discov
Gilani et al., 2016, UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer., Clin. Cancer Res.
Mpakou et al., 2013, Dasatinib inhibits proliferation and induces apoptosis in the KASUMI-1 cell line bearing the t(8;21)(q22;q22) and the N822K c-kit mutation., Leuk. Res.
Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
Hong et al., 2012, [Secondary mutation of c-kit/PDGFRα genotypes after imatinib mesylate therapy and its relationship with efficacy of sunitinib]., Zhonghua Bing Li Xue Za Zhi
Carvajal et al., 2011, KIT as a therapeutic target in metastatic melanoma., JAMA
Verstovsek et al., 2008, Phase II study of dasatinib in Philadelphia chromosome-negative acute and chronic myeloid diseases, including systemic mastocytosis., Clin. Cancer Res.
Tornillo et al., 2006, An update on molecular genetics of gastrointestinal stromal tumours., J. Clin. Pathol.
Cairoli et al., 2006, Prognostic impact of c-KIT mutations in core binding factor leukemias: an Italian retrospective study., Blood
Nakagomi et al., 2007, Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation., Lab. Invest.
Gleixner et al., 2007, Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT., Haematologica
Pan et al., 2007, EXEL-0862, a novel tyrosine kinase inhibitor, induces apoptosis in vitro and ex vivo in human mast cells expressing the KIT D816V mutation., Blood
Todd et al., 2013, Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells., Pigment Cell Melanoma Res
Gotlib et al., 2005, Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation., Blood
Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
Ustun et al., 2009, Chemotherapy and dasatinib induce long-term hematologic and molecular remission in systemic mastocytosis with acute myeloid leukemia with KIT D816V., Leuk. Res.
Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.
Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
Carlino et al., 2014, Resistance to c-Kit inhibitors in melanoma: insights for future therapies., Oncoscience
Dizdar et al., 2008, Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines., Breast Cancer Res. Treat.
Shah et al., 2006, Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis., Blood
Antonescu et al., 2007, L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition., Int. J. Cancer
Emile et al., 2012, Frequencies of KIT and PDGFRA mutations in the MolecGIST prospective population-based study differ from those of advanced GISTs., Med. Oncol.
Marcucci G et al., 2020, Combination of dasatinib with chemotherapy in previously untreated core binding factor acute myeloid leukemia: CALGB 10801., Blood Adv
Fiskus et al., 2006, Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells., Clin. Cancer Res.
Nam et al., 2007, Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells., Mol. Cancer Ther.
Chen et al., 2006, Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib)., Mol. Pharmacol.
Zhang et al., 2006, New assignments for multitasking signal transduction inhibitors., Mol. Pharmacol.
Ishibashi T et al., 2016, Ph-like ALL-related novel fusion kinase ATF7IP-PDGFRB exhibits high sensitivity to tyrosine kinase inhibitors in murine cells., Exp Hematol
Zhang G et al., 2017, Acute Lymphoblastic Leukemia Patient with Variant ATF7IP/PDGFRB Fusion and Favorable Response to Tyrosine Kinase Inhibitor Treatment: A Case Report., Am J Case Rep
Kneidinger M et al., 2008, The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils., Blood
Javadi et al., 2013, CBL linker region and RING finger mutations lead to enhanced granulocyte-macrophage colony-stimulating factor (GM-CSF) signaling via elevated levels of JAK2 and LYN., J. Biol. Chem.
Margutti et al., 2007, Are MAP kinases drug targets? Yes, but difficult ones., ChemMedChem
Trevino et al., 2006, Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model., Am. J. Pathol.
Shen et al., 2015, c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers., Cancer Res.
Ambrogio et al., 2016, Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma., Nat. Med.
Das et al., 2006, 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor., J. Med. Chem.
Shah NP et al., 2004, Overriding imatinib resistance with a novel ABL kinase inhibitor., Science
Nautiyal et al., 2011, Curcumin enhances dasatinib-induced inhibition of growth and transformation of colon cancer cells., Int. J. Cancer
Dunn et al., 2011, Dasatinib sensitizes KRAS mutant colorectal tumors to cetuximab., Oncogene
Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
Parseghian et al., 2017, Dual Inhibition of EGFR and c-Src by Cetuximab and Dasatinib Combined with FOLFOX Chemotherapy in Patients with Metastatic Colorectal Cancer., Clin. Cancer Res.
Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.
Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics
Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A
Miller et al., 2016, Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib., Mol. Cancer Ther.
Natsume H et al., 2012, The CRKL gene encoding an adaptor protein is amplified, overexpressed, and a possible therapeutic target in gastric cancer., J Transl Med

DASATINIB ABL2

Interaction Score: 1.21

Interaction Types & Directionality:

multitarget

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
20072833 17016423 11752352 25207766

Sources:
TdgClinicalTrial TEND CIViC
DASATINIB STAT5B

Interaction Score: 1.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
17020995 17431118

Sources:
TdgClinicalTrial TEND
DASATINIB CRKL

Interaction Score: 0.86

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22591714

Sources:
CIViC
DASATINIB DDR2

Interaction Score: 0.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration DDR2:S768R

Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs:
23932362 18938156 22328973

Sources:
CGI DoCM CIViC MyCancerGenomeClinicalTrial
DASATINIB EPHA2

Interaction Score: 0.67

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
20360610 20072833 17016423 17139284 19861960 19010823 18047674

Sources:
DTC TdgClinicalTrial ChemblInteractions CGI TEND DoCM MyCancerGenomeClinicalTrial
DASATINIB ABL1

Interaction Score: 0.55

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
25207766 24367893 26758680 18818391 15705718 25686603 16772610 19779040 16775234 20537386 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040 17016423 11752352 17701954 18191450

Sources:
MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB
DASATINIB KIT

Interaction Score: 0.45

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Clinical Status preclinical

Clinical Status early trials

PMIDs:
15685537 23149070 17699867 22932406 21642685 18559612 16731599 16384925 17259998 18024392 16912224 23582185 15972446 23714533 18986703 21689725 19164557 22504184 25157968 24045550 16397263 19671763 25594040 17351742 16434489 17372901 21953054 32092139

Sources:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM CIViC CancerCommons MyCancerGenomeClinicalTrial
DASATINIB IDH2

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type intrahepatic cholangiocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CGI
DASATINIB CBL

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
23696637

Sources:
CGI DoCM
DASATINIB TEC

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DTC
DASATINIB ABI1

Interaction Score: 0.43

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DASATINIB SIK3

Interaction Score: 0.43

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DASATINIB SIK1

Interaction Score: 0.43

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DASATINIB SRC

Interaction Score: 0.3

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction SRC inhibitor

Novel drug target Established target

PMIDs:
16230377 17429625 17155893 16397263 11752352 17148760 19462975 25835317 27222538 19098899 27231123 27154914

Sources:
TALC DTC TdgClinicalTrial JAX-CKB ChemblInteractions TEND GuideToPharmacology CancerCommons TTD
DASATINIB ARID1A

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27364904

Sources:
CIViC
DASATINIB BCR

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes Targets BCR-ABL fusion protein

Fusion protein BCR:ABL1

PMIDs:
15256671

Sources:
TALC PharmGKB FDA
DASATINIB PDGFRA

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 22328973 27582545

Sources:
DTC JAX-CKB CGI DoCM CIViC OncoKB
DASATINIB SRMS

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DASATINIB FGR

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
ChemblInteractions
DASATINIB FYN

Interaction Score: 0.19

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dasatinib, BMS-354825,Sprycel

Mechanism of Interaction SRC inhibitor

PMIDs:
20072833 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
DASATINIB BRAF

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect reduced kinase activity

Pathway activation

PMIDs:
20350999 21129611 22310681 25157968 19537845 18186519 26619011 12460919 12460918 21483012 19238210 22649091 12068308 23833300 19010912 23242808 27222538

Sources:
JAX-CKB CGI DoCM MyCancerGenomeClinicalTrial
DASATINIB FES

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB SIK2

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
DTC GuideToPharmacology
DASATINIB MAP3K10

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PDGFRB

Interaction Score: 0.12

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor beta inhibitor

Trial Name dasatinib, BMS-354825,Sprycel

PMIDs:
16436588 16497876 20072833 26703895 29133777

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND CIViC MyCancerGenomeClinicalTrial
DASATINIB CSF3R

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration CSF3R:Q741.,Y752.,W791.,T615A,T618I

PMIDs:
None found

Sources:
CGI
DASATINIB MAP3K20

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DTC
DASATINIB PTK6

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB LCK

Interaction Score: 0.1

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

Mechanism of Interaction SRC inhibitor

PMIDs:
20072833 17154512 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
DASATINIB CDC42BPA

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB APC

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
20473900

Sources:
JAX-CKB
DASATINIB HCK

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DASATINIB DYRK3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB FRK

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
ChemblInteractions
DASATINIB KRAS

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
20956938 27222538 26725216 28280091 27231123 26855149

Sources:
JAX-CKB CIViC
DASATINIB HRAS

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Response Type resistant

combination therapy Dasatinib + SCH772984

PMIDs:
27222538

Sources:
JAX-CKB
DASATINIB BTK

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DTC
DASATINIB IRAK4

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ACVR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TNK2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PKN2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB NF1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration NF1:del

Alteration NF1:.

PMIDs:
None found

Sources:
CGI
DASATINIB LYN

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
ChemblInteractions
DASATINIB LIMK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB AXL

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PLK4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MINK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB YES1

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

Mechanism of Interaction SRC inhibitor

PMIDs:
17541990 20072833 16507911

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND
DASATINIB SYK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TAOK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ABCG2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24322003

Sources:
PharmGKB
DASATINIB SLK

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP4K5

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB BLK

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction SRC inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
DASATINIB MAPK14

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DTC
DASATINIB ERBB4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP2K2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP2K1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MET

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26483207

Sources:
JAX-CKB
DASATINIB AURKB

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB CSF1R

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
DASATINIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB JAK2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PIK3CA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
26855149

Sources:
JAX-CKB
DASATINIB EGFR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Osimertinib

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
28416483

Sources:
JAX-CKB
DASATINIB FGFR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type chondrosarcoma

Response Type resistant

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CGI CIViC
DASATINIB PPARD

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB KDR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ERBB2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TP53

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
26855149

Sources:
JAX-CKB
DASATINIB SMAD3

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

CancerCommons: DASATINIB
- Version: 25-July-2013
Alternate Names:

3062316 PubChem Drug ID

Sprycel Drug Development Name

Sprycel Drug Trade Name

Drug Info:

Drug Class Kit Inhibitor

Source Reported Drug Name(s) Dasatinib

Pharmaceutical Developer Bristol-Myers Squibb

Publications:
MyCancerGenome: DASATINIB
- Version: 20-Jun-2017
Alternate Names:

BMS-354825 Development Name

SPRYCEL Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive), Acute lymphoblastic leukemia (Ph +)

Publications:
TdgClinicalTrial: DASATINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:
TEND: DASATINIB
- Version: 01-August-2011
Alternate Names:

Drug Info:

Drug Class antineoplastic agents, protein kinase inhibitors

Year of Approval 2006

Publications:

DTC: DASATINIB

Version: 02-September-2020

Alternate Names:

CHEMBL1421 ChEMBL Drug ID

Drug Info:

Publications:

Getlik M et al., 2009, Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc., J Med Chem

Zhang CH et al., 2015, Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer., J Med Chem

Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A

JAX-CKB: Dasatinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Saha et al., 2016, Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma., Cancer Discov

Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.

Gleixner et al., 2007, Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT., Haematologica

CGI: Dasatinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.

Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer

Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.

PharmGKB: dasatinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics

DoCM: DASATINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.

Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology

Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

CIViC: DASATINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.

Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med

Burgess MR et al., 2005, Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance., Proc Natl Acad Sci U S A

TALC: DASATINIB
- Version: 12-May-2016
Alternate Names:

BMS-354825 Drug Synonym

SPRYCEL Drug Trade Name

Drug Info:

Publications:
TTD: Dasatinib
- Version: 2020.06.01
Alternate Names:

D0E6XR TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1421
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 178102305
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: DASATINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1421
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
OncoKB: Dasatinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
FDA: Dasatinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
COSMIC: Dasatinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	dasatinib, BMS-354825,Sprycel
Novel drug target	Established target

Drug family	BCR-ABL inhibitor 2nd gen
Alteration	DDR2:S768R
Alteration	DDR2:I638F,L239R,G253C,G774V,L63V,G505S

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

combination therapy	[Nilotinib,Dasatinib]
Drug family	[BCR-ABL inhibitor 2nd gen]
Alteration	ABL1:T315I

Reported Cancer Type	Melanoma
Clinical Status	preclinical
Clinical Status	early trials

Indication/Tumor Type	intrahepatic cholangiocarcinoma
Response Type	sensitive
Approval Status	Preclinical

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Direct Interaction	yes
Mechanism of Interaction	SRC inhibitor
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	Platelet-derived growth factor receptor beta inhibitor
Trial Name	dasatinib, BMS-354825,Sprycel

Indication/Tumor Type	colorectal cancer
Response Type	sensitive
Approval Status	Preclinical

antagonist (inhibitory)
inhibitor (inhibitory)

multitarget
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

multitarget
inhibitor (inhibitory)

combination therapy	Dasatinib + Demcizumab
Indication/Tumor Type	lung adenocarcinoma
Response Type	sensitive

Approval Status	Preclinical - Cell line xenograft
Response Type	resistant
combination therapy	Dasatinib + SCH772984

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	predicted – sensitive
Approval Status	Preclinical - Cell culture

combination therapy	Dasatinib + Osimertinib
Indication/Tumor Type	lung cancer
Response Type	sensitive

Indication/Tumor Type	chondrosarcoma
Response Type	resistant
Approval Status	Preclinical

3062316	PubChem Drug ID
Sprycel	Drug Development Name
Sprycel	Drug Trade Name

DASATINIB Drug Record

DASATINIB chembl:CHEMBL1421 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: multitarget

Interaction Info: Trial Name dasatinib, BMS-354825,Sprycel Novel drug target Established target

PMIDs: 20072833 17016423 11752352 25207766

Sources: TdgClinicalTrial TEND CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name dasatinib, BMS-354825,Sprycel Novel drug target Established target

PMIDs: 17020995 17431118

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22591714

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family BCR-ABL inhibitor 2nd gen Alteration DDR2:S768R Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs: 23932362 18938156 22328973

Sources: CGI DoCM CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Clinical Status preclinical Pathway activation Variant Effect gain-of-function

PMIDs: 20360610 20072833 17016423 17139284 19861960 19010823 18047674

Sources: DTC TdgClinicalTrial ChemblInteractions CGI TEND DoCM MyCancerGenomeClinicalTrial

Interaction Types & Directionality: multitarget inhibitor (inhibitory)

Interaction Info: combination therapy [Nilotinib,Dasatinib] Drug family [BCR-ABL inhibitor 2nd gen] Alteration ABL1:T315I

PMIDs: 25207766 24367893 26758680 18818391 15705718 25686603 16772610 19779040 16775234 20537386 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040 17016423 11752352 17701954 18191450

Sources: MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Reported Cancer Type Melanoma Clinical Status preclinical Clinical Status early trials

PMIDs: 15685537 23149070 17699867 22932406 21642685 18559612 16731599 16384925 17259998 18024392 16912224 23582185 15972446 23714533 18986703 21689725 19164557 22504184 25157968 24045550 16397263 19671763 25594040 17351742 16434489 17372901 21953054 32092139

Sources: TALC TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM CIViC CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type intrahepatic cholangiocarcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 27231123

Sources: JAX-CKB CGI

Interaction Types & Directionality: n/a

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status preclinical

PMIDs: 23696637

Sources: CGI DoCM

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17684099

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: multitarget inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction SRC inhibitor Novel drug target Established target

PMIDs: 16230377 17429625 17155893 16397263 11752352 17148760 19462975 25835317 27222538 19098899 27231123 27154914

Sources: TALC DTC TdgClinicalTrial JAX-CKB ChemblInteractions TEND GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27364904

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Targets BCR-ABL fusion protein Fusion protein BCR:ABL1

PMIDs: 15256671

Sources: TALC PharmGKB FDA

Interaction Types & Directionality: n/a

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status preclinical

PMIDs: 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 22328973 27582545

Sources: DTC JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction SRC inhibitor Direct Interaction yes

PMIDs: None found

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction SRC inhibitor Direct Interaction yes

PMIDs: 18180381

Interaction Types & Directionality:

multitarget

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
20072833 17016423 11752352 25207766

Sources:
TdgClinicalTrial TEND CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
17020995 17431118

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
22591714

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration DDR2:S768R

Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs:
23932362 18938156 22328973

Sources:
CGI DoCM CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
20360610 20072833 17016423 17139284 19861960 19010823 18047674

Sources:
DTC TdgClinicalTrial ChemblInteractions CGI TEND DoCM MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
25207766 24367893 26758680 18818391 15705718 25686603 16772610 19779040 16775234 20537386 21895409 20367437 15381060 23676790 19466505 15256422 24456693 20697894 19652056 14745431 25157968 18615627 14559829 11853795 11964322 21505103 12399961 21562040 17016423 11752352 17701954 18191450

Sources:
MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM COSMIC CIViC GuideToPharmacology PharmGKB FDA OncoKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Reported Cancer Type Melanoma

Clinical Status preclinical

Clinical Status early trials

PMIDs:
15685537 23149070 17699867 22932406 21642685 18559612 16731599 16384925 17259998 18024392 16912224 23582185 15972446 23714533 18986703 21689725 19164557 22504184 25157968 24045550 16397263 19671763 25594040 17351742 16434489 17372901 21953054 32092139

Sources:
TALC TdgClinicalTrial JAX-CKB ChemblInteractions CGI TEND DoCM CIViC CancerCommons MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type intrahepatic cholangiocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CGI

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
23696637

Sources:
CGI DoCM

Interaction Types & Directionality:

n/a

PMIDs:
17684099

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction SRC inhibitor

Novel drug target Established target

PMIDs:
16230377 17429625 17155893 16397263 11752352 17148760 19462975 25835317 27222538 19098899 27231123 27154914

Sources:
TALC DTC TdgClinicalTrial JAX-CKB ChemblInteractions TEND GuideToPharmacology CancerCommons TTD

Interaction Types & Directionality:

n/a

PMIDs:
27364904

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes Targets BCR-ABL fusion protein

Fusion protein BCR:ABL1

PMIDs:
15256671

Sources:
TALC PharmGKB FDA

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 22328973 27582545

Sources:
DTC JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
ChemblInteractions

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dasatinib, BMS-354825,Sprycel

Mechanism of Interaction SRC inhibitor

PMIDs:
20072833 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect reduced kinase activity

Pathway activation

PMIDs:
20350999 21129611 22310681 25157968 19537845 18186519 26619011 12460919 12460918 21483012 19238210 22649091 12068308 23833300 19010912 23242808 27222538

Sources:
JAX-CKB CGI DoCM MyCancerGenomeClinicalTrial