PLX7904

PLX7904CAS号: 1393465-84-3分子式: C24H22F2N6O3S分子量: 512.53描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

PLX7904是一种有效的、选择性RAF抑制剂。它能够在BRAF突变的黑色素瘤细胞中有效地抑制ERK1/2的激活,但在表达突变RAS的细胞中并不过度激活ERK1/2。

纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
PB04
可溶性/溶解性
DMSO : ≥ 30 mg/mL (58.53 mM)
生物活性
靶点
Raf
In vitro(体外研究)
PLX7940 is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.Consistent with ERK1/2 re-activation driving the re-acquisition of malignant properties, PLX7904 promotes apoptosis and inhibits entry into S phase and anchorage-independent growth in mutant N-RAS mediated vemurafenib-resistant cells.PLX7904 is also evaluated in the human SCC cell line A431 and the human breast adenocarcinoma cell line SKBR3 as these cells achieve MAPK pathway activation by upstream signals feeding into RAS (through overexpression of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), respectively).
In vivo(体内研究)
PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.

分子结构图

PLX7904