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编 号：F756924
分子式：C20H23ClFN5O2S2
分子量：484.01
分子式：C20H23ClFN5O2S2
分子量：484.01
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CAS No: 2923700-82-5
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生物活性：
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
体内研究：
Everafenib (50 mg/kg; IP; once daily, for 5 days) increases median survival of melanoma mice from 39 to 50.5 days.Animal Model:Female athymic nude mice (intracranially injected with 5×104 A375 melanoma cells)
Dosage:50 mg/kg
Administration:IP; once daily, for 5 days
Result:Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib (HY-14660).
体外研究：
Everafenib (1-10 μM; 1 or 24 h) inhibits MAPK signaling in A375 cells.
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
体内研究：
Everafenib (50 mg/kg; IP; once daily, for 5 days) increases median survival of melanoma mice from 39 to 50.5 days.Animal Model:Female athymic nude mice (intracranially injected with 5×104 A375 melanoma cells)
Dosage:50 mg/kg
Administration:IP; once daily, for 5 days
Result:Increased median survival from 39 to 50.5 days, and outperformed Dabrafenib (HY-14660).
体外研究：
Everafenib (1-10 μM; 1 or 24 h) inhibits MAPK signaling in A375 cells.
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