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XL-888
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。
XL-888图片
CAS NO:1149705-71-4
规格:98%
分子量:503.64
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Hsp90 inhibitor
CAS:1149705-71-4
分子式:C29H37N5O3
分子量:503.64
纯度:98%
存储:Store at -20°C

Background:

XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with values of 50% inhibition concentration IC50of 22 nM and 44 nM respectively. It also exerts considerably weaker inhibition against a range of other diverse kinases with IC50more than 3600 nM for all. X-ray crystallographic analysis reveals that the XL-888 binds to HSP90 through the formation of H-bonding between the N-(R)-sec-butylanthranilamide moiety of XL-888 and ASP93 of HSP90. In recent studies, XL-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of IC50ranging from 0.1 nM to 45.5 nM.


Reference


[1].Paraiso KH, Haarberg HE, Wood E, Rebecca VW, Chen YA, Xiang Y, Ribas A, Lo RS, Weber JS, Sondak VK, John JK, Sarnaik AA, Koomen JM, Smalley KS. The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms. Clin Cancer Res. 2012; 18(9):2502-2514
[2].Bussenius J, Blazey CM, Aay N, Anand NK, Arcalas A, Baik T, Bowles OJ, Buhr CA, Costanzo S, Curtis JK, DeFina SC, Dubenko L, Heuer TS, Huang P, Jaeger C, Joshi A, Kennedy AR, Kim AI, Lara K, Lee J, Li J, Lougheed JC, Ma S, Malek S, Manalo JC, Martini JF, McGrath G, Nicoll M, Nuss JM, Pack M, Peto CJ, Tsang TH, Wang L, Womble SW, Yakes M, Zhang W, Rice KD. Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. Bioorg Med Chem Lett. 2012; 22(17): 5396-5404.