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DASATINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • 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
    (13 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: 1.55

    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: 1.18

    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   DDR2

    Interaction Score: 1.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    23932362 18938156 22328973


    Sources:
    DoCM CIViC MyCancerGenomeClinicalTrial

  • DASATINIB   CRKL

    Interaction Score: 0.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22591714


    Sources:
    CIViC

  • DASATINIB   TEC

    Interaction Score: 0.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17684099


    Sources:
    DTC

  • DASATINIB   EPHA2

    Interaction Score: 0.68

    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 TEND DoCM MyCancerGenomeClinicalTrial

  • DASATINIB   ABL1

    Interaction Score: 0.58

    Interaction Types & Directionality:
    multitarget
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name dasatinib, BMS-354825,Sprycel
    Novel drug target Established target
    Clinical Status NCCN guidelines

    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 TEND DoCM COSMIC CIViC PharmGKB FDA OncoKB

  • DASATINIB   KIT

    Interaction Score: 0.54

    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 TEND DoCM CIViC CancerCommons MyCancerGenomeClinicalTrial

  • DASATINIB   ABI1

    Interaction Score: 0.44

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DASATINIB   ARID1A

    Interaction Score: 0.35

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27364904


    Sources:
    CIViC

  • DASATINIB   SRC

    Interaction Score: 0.32

    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 CancerCommons TTD

  • DASATINIB   IDH2

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27231123


    Sources:
    JAX-CKB

  • 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   CBL

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    23696637


    Sources:
    DoCM

  • DASATINIB   FGR

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction SRC inhibitor
    Direct Interaction yes

    PMIDs:
    18180381


    Sources:
    ChemblInteractions

  • 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 DoCM CIViC OncoKB

  • DASATINIB   FES

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • 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   FYN

    Interaction Score: 0.21

    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 DoCM MyCancerGenomeClinicalTrial

  • DASATINIB   MAP3K10

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   PDGFRB

    Interaction Score: 0.14

    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   LCK

    Interaction Score: 0.12

    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   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   CDC42BPA

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   SIK2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   HCK

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction SRC inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    DTC ChemblInteractions

  • 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   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   BTK

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17684099


    Sources:
    DTC

  • 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   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   IRAK4

    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   ACVR1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • 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   PKN2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   LIMK1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   AXL

    Interaction Score: 0.04

    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   SYK

    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   SLK

    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   MAP4K5

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   ERBB4

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   BLK

    Interaction Score: 0.03

    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   MAP2K2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   CSF1R

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    TALC

  • 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: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • 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   KDR

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • DASATINIB   PPARD

    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 CIViC

  • 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 Trade Name
    Sprycel Drug Development 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

  • 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:
    SPRYCEL Drug Trade Name
    BMS-354825 Drug Synonym

    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:

  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21