XL-888

Catalog #
27781-1
$320 *
Size: 10 mg
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Description

XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with IC50s of 22 nM and 44 nM respectively. It also exerts considerably weaker inhibition against a range of other diverse kinases with IC50 more than 3600 nM for all. In recent studies, XL-888 has exhibits strong anti-proliferative activities in a panel of tumor cells with values of IC50 ranging from 0.1 nM to 45.5 nM.

Synonyms
Xl 888; Xl888; 2-(butan-2-ylamino)-4-N-[(1R,5S)-8-[5-(cyclopropanecarbonyl)pyridin-2-yl]-8-azabicyclo[3.2.1]octan-3-yl]-5-methylbenzene-1,4-dicarboxamide
Product Info
Storage and Usage
Citations
Target(s)
HSP90
Formula
C29H37N5O3
MW
503.6 Da
Solubility
Soluble in DMSO
CAS Registry #
1149705-71-4
Background
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.
References
1. Paraiso KH, et al. Clin Cancer Res. 2012; 18(9):2502-2514.
2. Bussenius J, et al. Bioorg Med Chem Lett. 2012; 22(17): 5396-5404.