Vemurafenib (PLX4032, RG7204)

Short Summary : BRAF kinase inhibitor

Category : MAPK Signaling|MEK1/2

Purity : 0.9833

CAS Number : 918504-65-1

Formula : C23H18ClF2N3O3S

Molecular Weight : 489.93

SMILE : CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)Cl)F

Solubility : >24.5mg/mL in DMSO

Storage : Store at -20°C

Description : Vemurafenib is an inhibitor of BRAF kinase. It inhibits BRAFV600E and also has inhibitory activity in vitro against several other kinds of kinases, including CRAF, ARAF and wild-type BRAF. Vemurafenib is a competitive small-molecule serine–threonine kinase inhibitor that functions by binding to the ATP-binding domain of mutant BRAF. Vemurafenib can also give rise to activation of downstream MEK by normal RAF homo- and heterodimers in non-BRAF mutated cells, which has been shown to be caused by transactivation of the nondrug-bound partner in BRAF to CRAF heterodimers and CRAF to CRAF homodimers.
Reference
Keith. T Flaherty, Uma Yasothan and Peter Kirkpatrick. Vemurafenib. Nature Reviews Drug Discovery. 2011; 10: 811 – 812.
Jason J. Luke, F. Stephen Hodi. Vemurafenib and BRAF Inhibition: A New Class of Treatment for Metastatic Melanoma. Clinical Cancer Research. 2012; 18: 9 – 14.

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