Vemurafenib

Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

Product Specifications

CAS Number

[918504-65-1]

Product Name Alternative

PLX4032; RG7204; RO5185426

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Raf

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Vemurafenib.html

Purity

99.85

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

FC1=CC=C(C(F)=C1C(C2=CNC3=NC=C(C=C32)C4=CC=C(C=C4)Cl)=O)NS(CCC)(=O)=O

Molecular Formula

C23H18ClF2N3O3S

Molecular Weight

489.92

Precautions

H302, H315, H319, H335

References & Citations

[1]Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467 (7315), 596-599.|[2]Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70 (13), 5518-5527.|[3]Prahallad A, et al. Unresponsiveness of colon cancer to BRAF (V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483 (7387), 100-103.|[4]Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6 (4) :361-5.|[5]Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102 (2) :634-643.