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Vemurafenib

CAS No. : 918504-65-1

MCE 国际站：Vemurafenib

产品活性：Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的，有效的 B-RAF 选择性抑制剂，能够抑制 RAF^V600E 和 c-RAF-1 的活性，IC₅₀ 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：Raf  |  Autophagy

In Vitro: Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells. RG7204 is a potent inhibitor of proliferation in those expressing RAF^V600E but not BRAF^WT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032.

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. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts.

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