您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > LGX818
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
LGX818
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。
LGX818图片
CAS NO:1269440-17-6
规格:98%
分子量:540.01
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
RAF inhibitor,potent and selective
CAS:1269440-17-6
分子式:C22H27ClFN7O4S
分子量:540.01
纯度:98%
存储:Store at -20°C

Background:

LGX818 is a potent and selective inhibitor of RAF kinase with EC50 value of 3nM in A375 cells [1].


The V600E mutation of B-Raf in the kinase domain results in constitutive activation of B-Raf and promotes cancer development. LGX818 is a RAF kinase inhibitor targeting V600E mutant B-Raf. It has little effect against wild-type BRAF. LGX818 has selective anti-proliferative and apoptotic activity ion in cells expressing BRAFV600E. It shows no significant activity against a panel of 100 kinases and no suppression of cell growth with more than 400 cell lines expressing BRAFV600E. In the A375 human melanoma cell line, LGX818 inhibits the phospho-ERK with EC50 value of 3nM and causes subsequent cell proliferation inhibition with EC50 value of 4nM. In human melanoma xenograft models, oral administration of LGX818 shows strong decrease in phospho-MEK and induces tumor regression [1, 2].


参考文献:
[1] Stuart D D, Li N, Poon D J, et al. Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor. Cancer Research, 2012, 72(8 Supplement): 3790.
[2] Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol, 2013, 6(1): 30.