DGIdb - PLX-4720 Drug Record

PLX-4720 chembl:CHEMBL1230020 Antineoplastic

Alternate Names:

PLX-4720
PLX 4720
N-{3-[(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-3-YL)CARBONYL]-2,4-DIFLUOROPHENYL}PROPANE-1-SULFONAMIDE
PLX4720
N-[3-(5-CHLORO-1H-PYRROLO[2,3-B]PYRIDINE-3-CARBONYL)-2,4-DIFLUOROPHENYL]PROPANE-1-SULFONAMIDE
chemidplus:918505-84-7
chembl:CHEMBL1230020
pubchem.compound:24180719
drugbank:06999

Drug Info:

(0 More Sources)

Publications:

Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov
Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
Wagle et al., 2011, Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling., J. Clin. Oncol.
Prahallad et al., 2012, Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR., Nature
Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
Karoulia et al., 2016, An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling., Cancer Cell
Frederick et al., 2014, Clinical profiling of BCL-2 family members in the setting of BRAF inhibition offers a rationale for targeting de novo resistance using BH3 mimetics., PLoS ONE
Vinik et al., 2016, Patient-Reported Outcomes and Quality of Life with Sunitinib Versus Placebo for Pancreatic Neuroendocrine Tumors: Results From an International Phase III Trial., Target Oncol
Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
Lerner et al., 2015, Targeting a Plk1-Controlled Polarity Checkpoint in Therapy-Resistant Glioblastoma-Propagating Cells., Cancer Res.
Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
Tsai et al., 2008, Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity., Proc. Natl. Acad. Sci. U.S.A.
Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell
Ghosh C et al., 2020, A Combinatorial Strategy for Targeting <i>BRAF</i> <sup>V600E</sup>-Mutant Cancers with BRAF<sup>V600E</sup> Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res
Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Posch et al., 2013, Combined targeting of MEK and PI3K/mTOR effector pathways is necessary to effectively inhibit NRAS mutant melanoma in vitro and in vivo., Proc. Natl. Acad. Sci. U.S.A.
Girotti et al., 2015, Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma., Cancer Cell
Turajlic et al., 2014, Whole-genome sequencing reveals complex mechanisms of intrinsic resistance to BRAF inhibition., Ann. Oncol.
Lionarons DA et al., 2019, RAC1<sup>P29S</sup> Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance., Cancer Cell
Johannessen et al., 2013, A melanocyte lineage program confers resistance to MAP kinase pathway inhibition., Nature

PLX-4720 PTPN11

Interaction Score: 1.96

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26351322

Sources:
JAX-CKB
PLX-4720 RAC1

Interaction Score: 1.72

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31257073

Sources:
CIViC
PLX-4720 BRAF

Interaction Score: 1.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources:
JAX-CKB CIViC
PLX-4720 GNAQ

Interaction Score: 1.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24504448

Sources:
CIViC
PLX-4720 NRAS

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
23431193 25500121

Sources:
JAX-CKB
PLX-4720 MAP2K1

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical

PMIDs:
19915144 21383288

Sources:
JAX-CKB
PLX-4720 MITF

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24185007

Sources:
CIViC
PLX-4720 PTEN

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
24265153

Sources:
JAX-CKB
PLX-4720 YES1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

JAX-CKB: PLX4720

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Van Allen et al., 2014, The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma., Cancer Discov

Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.

Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med

CIViC: PLX4720

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Sievert AJ et al., 2013, Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas., Proc Natl Acad Sci U S A

Ghosh C et al., 2020, A Combinatorial Strategy for Targeting BRAF V600E-Mutant Cancers with BRAFV600E Inhibitor (PLX4720) and Tyrosine Kinase Inhibitor (Ponatinib)., Clin Cancer Res

Rad et al., 2013, A genetic progression model of Braf(V600E)-induced intestinal tumorigenesis reveals targets for therapeutic intervention., Cancer Cell

DTC: PLX-4720
- Version: 02-September-2020
Alternate Names:

CHEMBL1230020 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1230020
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	colorectal cancer
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Indication/Tumor Type	melanoma
Response Type	resistant
Approval Status	Preclinical - Cell line xenograft

combination therapy	GDC-0941 + PLX4720
Indication/Tumor Type	melanoma
Response Type	sensitive

PLX-4720 Drug Record

PLX-4720 chembl:CHEMBL1230020 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 26351322

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31257073

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical - Cell line xenograft

PMIDs: 26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources: JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24504448

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical - Cell line xenograft

PMIDs: 23431193 25500121

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical

PMIDs: 19915144 21383288

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24185007

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy GDC-0941 + PLX4720 Indication/Tumor Type melanoma Response Type sensitive

PMIDs: 24265153

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

JAX-CKB: PLX4720

Alternate Names:

Drug Info:

CIViC: PLX4720

Alternate Names:

Drug Info:

DTC: PLX-4720

Alternate Names: CHEMBL1230020 ChEMBL Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1230020

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26351322

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
31257073

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
26351322 21383288 24265153 19915144 22281684 27217440 23242808 27523909 24983357 27924459 26461489 26573800 20538618 18287029 23845441 31937621 23533272 10592235

Sources:
JAX-CKB CIViC

Interaction Types & Directionality:

n/a

PMIDs:
24504448

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell line xenograft

PMIDs:
23431193 25500121

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical

PMIDs:
19915144 21383288

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
24185007

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy GDC-0941 + PLX4720

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
24265153

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

CHEMBL1230020 ChEMBL Drug ID