Everafenib 是一种有效且具有血脑屏障透过性的BRAF抑制剂，也抑制MAPK通路。Everafenib 对一系列V600EBRAF 黑色素瘤细胞系具有抑制活性，IC50范围为 2-10 nM，优于Dabrafenib 和Vemurafenib。Everafenib 能有效提高颅内转移性黑色素瘤小鼠模型的存活天数。

Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600E BRAF melanoma cell lines with IC 50 values of 2-10 nM, which is better than Dabrafenib and Vemurafenib. Everafenib has efficacy in an intracranial mouse model of metastatic melanoma [1].

Everafenib (1-10 μM; 1 or 24 h) inhibits MAPK signaling in A375 cells [1]. Western Blot Analysis [1] Cell Line: A375 ( V600E BRAF) Concentration: 0.01, 0.1, 1 and 10 μM Incubation Time: 1 or 24 h Result: Inhibited phospho-ERK1/2 in a dose-dependent manner, also inhibited phospho-MEK1/2.

Everafenib (50 mg/kg; IP; once daily, for 5 days) increases median survival of melanoma mice from 39 to 50.5 days [1]. Animal Model: Female athymic nude mice (intracranially injected with 5×10 4 A375 melanoma cells) [1] Dosage: 50 mg/kg Administration: IP; once daily, for 5 days Result: Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib.

C20H23ClFN5O2S2

484.01

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years