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LXH254
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LXH254图片
CAS NO:1800398-38-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
LXH254 是B/C Raf抑制剂,详细信息请参考专利文献 WO2018051306A1 中的化合物 A。

产品描述

LXH254 is a potent C-Raf and B-Raf inhibitor.

体外活性

LXH254 is an adenosine triphosphate (ATP)-competitive inhibitor of BRAF and CRAF protein kinases.?LXH254 is also referred to as a c-RAF (or CRAF) inhibitor or a C-RAF/c-Raf kinase inhibitor.?In cell-based assays, LXH254 has demonstrated anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling.?Moreover, LXH254 is a Type 2 ATP -competitive inhibitor of both B-Raf and C-Raf that keeps the kinase pocket in an inactive conformation, thereby reducing the paradoxical activation seen with many B-Raf inhibitors, and blocking mutant RAS-driven signaling and cell proliferation.

体内活性

LXH254 exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes.Treatment with LXH254 generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C).

Cas No.

1800398-38-2

分子式

C25H25F3N4O4

分子量

502.49

储存和溶解度

DMSO:100 mg/mL (199.01 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years