PLX-4032, B-Raf inhibitor (TBI2928)

Description

Product Details

Formal Name: N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

Alternate Names: Vemurafenib; R7204; Ro 51-85426

Molecular Formula: C₂₃H₁₈ClF₂N₃O₃S

Formula Weight: 489.92

CAS Number: 918504-65-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 100 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

B-Raf inhibitor

Functions

An ATP-competitive inhibitor of mutant V600E/F and wild type B-Raf, IC50s=31 and 100 nM respectively. 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. Inhibits the growth of B-Raf V600E-positive melanomas in vitro and in vivo. Treatment of patients that carry the V600E BRAF mutation resulted in complete or partial tumor regression.

Application Procedures

First dissolved in DMSO (up to 100 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.