Vemurafenib | CAS:918504-65-1

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のVemurafenib(CAS:918504-65-1)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:Vemurafenib; RG7204; R7204; RO5185426; PLX4032
Cat. No. :CS-0216
CAS No. :918504-65-1
Formula:C23H18ClF2N3O3S
M. Wt. : 489.92
Solubility:DMSO: 6.2 mg/mL

Vemurafenib is a novel and potent inhibitor of B-RAF kinase, with IC50 values of RAFV600E (31 nM) and c-RAF-1 (48 nM).IC50 & Target: IC50: 31 nM (BRAFV600E), 48 nM (c-RAF-1)In Vitro: Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].In Vivo: Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].

Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103. 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. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.