产品说明书

	同义名 :	-
	CAS号 :	1393466-87-9
	货号 :	A840010
	分子式 :	C25H21F3N6O3S
	纯度 :	99%+
	分子量 :	542.533
	MDL号 :	MFCD29472263
	存储条件：	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

PLX8394 is an orally active BRAF small molecule inhibitor with IC50 of 3.8 nM for BRAF(V600E), 14 nM for WT BRAF and 23 nM for CRAF. It has potential antitumor activity[1]. PLX8394 is a potent inhibition of ERK1/2 phosphorylation in cells at concentrations above 25 nM, and in parental cells at a lower threshold of 10 nM. This compound effectively diminishes levels of cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in both parental and PRT cells. Additionally, PLX8394 is capable of inhibiting ERK1/2 phosphorylation and growth in PLX4032-resistant cells that possess a BRAF V600K/L505H double mutation or a transposon-induced, N-terminal truncated form of BRAF[1]. PLX8394 also significantly reduces tumor cell growth and curtails MAPK signaling in LA cell lines harboring either the endogenous V600E mutation or non-V600 mutant forms of BRAF[2].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.84mL 0.37mL 0.18mL	9.22mL 1.84mL 0.92mL	18.43mL 3.69mL 1.84mL

参考文献
[1]Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-484. [2]Okimoto RA, et al. Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer. Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):13456-13461