Vemurafenib, Free Base (PLX4032, R7204, RG7204, RO5185426, Ro 51-85426, Zelboraf, CAS 918504-65-1), >99%

LC Laboratories' Product Number V-2800 - Vemurafenib, Free Base (PLX4032, R7204, RG7204, RO5185426, Ro 51-85426, Zelboraf, CAS 918504-65-1), >99% - for research use only. NOTE: As of September 2011 the current correct CAS number for vemurafenib, also known as PLX4032, is given above. Chemical Abstracts Service recently canceled another CAS number, 1029872-54-5, that had previously been used for vemurafenib under its older name, PLX4032. However, this canceled number remains in wide use and receives the vast majority of hits on Google. Vemurafenib inhibited ERK1/2 in the highly sensitive BRAF(V600E/K) cells, while it activated the pathway in the (resistant) BRAF(WT) cells. Using an IC50g cutoff of 1 µM, 13 of 35 cell lines tested showed sensitivity to vemurafenib, 16 were resistant, and 6 were intermediate in sensitivity. Vemurafenib caused growth inhibition, G0/G1 arrest, and apoptosis in the sensitive cell lines. A BRAF mutation favored but did not guarantee a sensitive response, while cells bearing a neuroblastoma RAS viral oncogene homolog mutation or wild-type BRAF were resistant. Vemurafenib inhibited the growth of B-Raf V600E-positive melanomas in vitro and in vivo. Vemurafenib selectively inhibited the RAF/MEK/ERK pathway in BRAF mutant cells and induced regression of BRAF mutant xenografts. However, no tumor regression occurred in patients until greater than 80% inhibition of ERK phosphorylation in the tumors was reached. Treatment of patients with metastatic melanoma that carry the V600E BRAF mutation with vemurafenib resulted in complete or partial tumor regression in the majority of patients. Vemurafenib is the active ingredient in the drug product sold under the trade name Zelboraf®. This drug is currently approved in at least one country for use in patients with late-stage melanoma. NOTE: The Vemurafenib, Free Base research compound sold by LC Laboratories is NOT Zelboraf®, and is NOT for human use.

• Supplier: LC Laboratories
• Product #: V-2800
• Sku #: V-2800_1g