Drug Information

Drug General Information
Drug ID
D0F5JZ
Former ID
DIB020738
Drug Name
PLX-4720
Synonyms
PLX 4720; PLX4720 (BRAF inhibitor)
Drug Type
Small molecular drug
Indication Cutaneous Melanoma [ICD10:C43-C44] Phase 1 [1572597]
Structure
Download
2D MOL
Formula
C17H14ClF2N3O3S
InChI
InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22)
InChIKey
YZDJQTHVDDOVHR-UHFFFAOYSA-N
PubChem Compound ID
24180719
PubChem Substance ID
48426216, 49663614, 56072661, 56412907, 84982168, 87557609, 99376103, 99437005, 99443470, 104246213, 124757038, 124898783, 125163842, 125748896, 126584082, 126626061, 126660697, 126728325, 131480707, 135263014, 135685180, 135685181, 135685200, 135686124, 135686125, 135686146, 135686147, 135697775, 135727403, 136367335, 136920368, 137275835, 138197513, 143499492, 152058490, 152237503, 152258869, 152344245, 160647718, 160968084, 162011355, 162202588, 162938881, 163685871, 164764472, 165238065, 172914381, 174561099, 177748742, 178102330
Drug Resistance Mutation (DRM)
DRM DRM Info
Target and Pathway
Target(s) mRNA of B-Raf Target Info Inhibitor [531679]
Vascular endothelial growth factor receptor 2 Target Info Inhibitor [526516]
KEGG Pathway MAPK signaling pathway
ErbB signaling pathway
Rap1 signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
FoxO signaling pathway
mTOR signaling pathway
Vascular smooth muscle contraction
Focal adhesion
Natural killer cell mediated cytotoxicity
Long-term potentiation
Neurotrophin signaling pathway
Serotonergic synapse
Long-term depression
Regulation of actin cytoskeleton
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Alcoholism
Hepatitis C
Pathways in cancer
Proteoglycans in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Thyroid cancer
Melanoma
Bladder cancer
Chronic myeloid leukemia
Acute myeloid leukemia
Non-small cell lung cancerhsa04014:Ras signaling pathway
Cytokine-cytokine receptor interaction
Endocytosis
PI3K-Akt signaling pathway
VEGF signaling pathway
NetPath Pathway IL-7 Signaling PathwayNetPath_14:IL2 Signaling Pathway
PANTHER Pathway Angiogenesis
Integrin signalling pathway
Interleukin signaling pathway
PDGF signaling pathway
T cell activation
VEGF signaling pathway
Ras Pathway
CCKR signaling map STP00005:Angiogenesis
Pathway Interaction Database CDC42 signaling events
mTOR signaling pathway
Ras signaling in the CD4+ TCR pathway
ErbB1 downstream signaling
PDGFR-beta signaling pathway
Signaling events mediated by VEGFR1 and VEGFR2
Trk receptor signaling mediated by the MAPK pathwayhif2pathway:HIF-2-alpha transcription factor network
Beta3 integrin cell surface interactions
Signaling events mediated by TCPTP
SHP2 signaling
S1P1 pathway
VEGF and VEGFR signaling network
Integrins in angiogenesis
Notch-mediated HES/HEY network
PathWhiz Pathway Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Reactome Spry regulation of FGF signaling
Frs2-mediated activation
ARMS-mediated activation
CREB phosphorylation through the activation of Ras
RAF activation
MAP2K and MAPK activation
Negative feedback regulation of MAPK pathway
Negative regulation of MAPK pathwayR-HSA-194306:Neurophilin interactions with VEGF and VEGFR
VEGF binds to VEGFR leading to receptor dimerization
Integrin cell surface interactions
EPHA-mediated growth cone collapse
VEGFA-VEGFR2 Pathway
VEGFR2 mediated cell proliferation
WikiPathways Serotonin Receptor 4/6/7 and NR3C Signaling
Serotonin HTR1 Group and FOS Pathway
Senescence and Autophagy in Cancer
Regulation of Actin Cytoskeleton
EGF/EGFR Signaling Pathway
MAPK Cascade
MAPK Signaling Pathway
Bladder Cancer
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Polycystic Kidney Disease Pathway
Corticotropin-releasing hormone
B Cell Receptor Signaling Pathway
Signaling Pathways in Glioblastoma
Integrated Breast Cancer Pathway
Signaling by FGFR
NGF signalling via TRKA from the plasma membrane
Integrin-mediated Cell AdhesionWP306:Focal Adhesion
Nifedipine Activity
Cardiac Progenitor Differentiation
Signaling by VEGF
Angiogenesis
References
Ref 1572597Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer.
Ref 526516In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37.
Ref 531679Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.

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