PLX-4032
BRAF inhibitor / An ATP-competitive inhibitor of mutant V600E/F and wild type B-Raf, IC50s=31 and 100 nM respectively.1 Induced growth inhibition, G0/G1 arrest and apoptosis in a variety of cancer cell lines, with a B-Raf mutation favoring but not guaranteeing a response.2 Inhibits the growth of B-Raf V600E-positive melanomas in vitro and in vivo.3 Treatment of patients that carry the V600E BRAF mutation resulted in complete or partial tumor regression.4
Biochemicals & reagents
918504-65-1
Vemurafenib; R7204; Ro 51-85426
1) Khazak et al. (2007), Selective Raf inhibition in cancer therapy; Expert Opin. Ther. Targets, 11 1587 2) Tap et al. (2010), Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma; Neoplasia, 12 637 3) Lee et al. (2010), PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas; Pigment Cell Melanoma Res., 23 820 4) Flaherty et al. (2010), Inhibition of mutated, activated BRAF in metastatic melanoma; N. Engl. J. Med., 363 809
-20°C
TARGET: Kinase -- PATHWAY: Cell cycle; Apoptosis inducer -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer