| 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 |
[1]
|
|---|
| 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 |
|
| 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 |
[2]
|
|---|
| Vascular endothelial growth factor receptor 2 |
Target Info |
Inhibitor |
[3]
|
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KEGG Pathway
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MAPK signaling pathway
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ErbB signaling pathway
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Rap1 signaling pathway
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cAMP signaling pathway
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Chemokine signaling pathway
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FoxO signaling pathway
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mTOR signaling pathway
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Vascular smooth muscle contraction
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Focal adhesion
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Natural killer cell mediated cytotoxicity
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Long-term potentiation
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Neurotrophin signaling pathway
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Serotonergic synapse
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Long-term depression
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Regulation of actin cytoskeleton
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Insulin signaling pathway
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Progesterone-mediated oocyte maturation
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Alcoholism
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Hepatitis C
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Pathways in cancer
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Proteoglycans in cancer
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Colorectal cancer
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Renal cell carcinoma
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Pancreatic cancer
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Endometrial cancer
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Glioma
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Prostate cancer
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Thyroid cancer
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Melanoma
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Bladder cancer
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Chronic myeloid leukemia
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Acute myeloid leukemia
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Non-small cell lung cancerhsa04014:Ras signaling pathway
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Cytokine-cytokine receptor interaction
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Endocytosis
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PI3K-Akt signaling pathway
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VEGF signaling pathway
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NetPath Pathway
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IL-7 Signaling PathwayNetPath_14:IL2 Signaling Pathway
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PANTHER Pathway
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Angiogenesis
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Integrin signalling pathway
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Interleukin signaling pathway
|
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PDGF signaling pathway
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T cell activation
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VEGF signaling pathway
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Ras Pathway
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CCKR signaling map STP00005:Angiogenesis
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Pathway Interaction Database
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CDC42 signaling events
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mTOR signaling pathway
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Ras signaling in the CD4+ TCR pathway
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ErbB1 downstream signaling
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PDGFR-beta signaling pathway
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Signaling events mediated by VEGFR1 and VEGFR2
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Trk receptor signaling mediated by the MAPK pathwayhif2pathway:HIF-2-alpha transcription factor network
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Beta3 integrin cell surface interactions
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Signaling events mediated by TCPTP
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SHP2 signaling
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S1P1 pathway
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VEGF and VEGFR signaling network
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Integrins in angiogenesis
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Notch-mediated HES/HEY network
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PathWhiz Pathway
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Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
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Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
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Reactome
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Spry regulation of FGF signaling
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Frs2-mediated activation
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ARMS-mediated activation
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CREB phosphorylation through the activation of Ras
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RAF activation
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MAP2K and MAPK activation
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Negative feedback regulation of MAPK pathway
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Negative regulation of MAPK pathwayR-HSA-194306:Neurophilin interactions with VEGF and VEGFR
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VEGF binds to VEGFR leading to receptor dimerization
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Integrin cell surface interactions
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EPHA-mediated growth cone collapse
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VEGFA-VEGFR2 Pathway
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VEGFR2 mediated cell proliferation
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WikiPathways
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Serotonin Receptor 4/6/7 and NR3C Signaling
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Serotonin HTR1 Group and FOS Pathway
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Senescence and Autophagy in Cancer
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Regulation of Actin Cytoskeleton
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EGF/EGFR Signaling Pathway
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MAPK Cascade
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MAPK Signaling Pathway
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Bladder Cancer
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Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
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Polycystic Kidney Disease Pathway
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Corticotropin-releasing hormone
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B Cell Receptor Signaling Pathway
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Signaling Pathways in Glioblastoma
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Integrated Breast Cancer Pathway
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Signaling by FGFR
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NGF signalling via TRKA from the plasma membrane
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Integrin-mediated Cell AdhesionWP306:Focal Adhesion
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Nifedipine Activity
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Cardiac Progenitor Differentiation
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Signaling by VEGF
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Angiogenesis
|
| References |
| REF 1 | Targeting BRAFV600E with PLX4720 displays potent antimigratory and anti-invasive activity in preclinical models of human thyroid cancer. |
|---|
| REF 2 | Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. |
|---|
| REF 3 | In 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. |
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