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Vemurafenib

维罗非尼,维罗菲尼,威罗菲尼,PLX-4032,PLX4032,RO5185426,PLX 4032,RO 5185426,RO-5185426,RO5185426

Vemurafenib (PLX4032, RG7204)是一种新型有效的B-RafV600E抑制剂，IC50为31 nM。

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生物活性

Vemurafenib is an inhibitor of BRAF kinase. It inhibits BRAFV600E and also has inhibitory activity in vitro against several other kinds of kinases, including CRAF, ARAF and wild-type BRAF. Vemurafenib is a competitive small-molecule serine–threonine kinase inhibitor that functions by binding to the ATP-binding domain of mutant BRAF. Vemurafenib can also give rise to activation of downstream MEK by normal RAF homo- and heterodimers in non-BRAF mutatedcells, which has been shown to be caused by transactivation of the nondrug-bound partner in BRAF to CRAF heterodimers and CRAF to CRAF homodimers.
体外研究
体内研究
激酶实验
细胞实验

0–10 μM
动物实验

12.5 mg/kg–100 mg/kg 口服饲喂，每天两次
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Bollag G, et al. Nature, 2010, 467(7315), 596-599.

分子式 C23H18ClF2N3O3S	分子量 489.92	CAS号 918504-65-1	储存方式 ﹣20 ℃冷藏长期储存。冰袋运输
溶剂（常温）	DMSO ≥96 mg/mL	Water Insoluble	Ethanol Insoluble

体内溶解度
30% PEG400+0.5% Tween80+5% Propylene glycol

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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