货号 | 16309-25mg |
描述 | Heat shock protein 90 (Hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis.1 XL888 is an ATP-competitive inhibitor of Hsp90.2 Through this action, specific client proteins are degraded, resulting in cell cycle arrest or apoptosis.3,4,5 XL888 is orally bioavailable and shows efficacy in tumor regression in gastric carcinoma and melanoma xenografts in mice.2,4 |
供应商 | Cayman |
应用文献 | |
1.Taldone, T.,Sun, W. and Chiosis, G. Discovery and development of heat shock protein 90 inhibitors. Bioorganic & Medicinal Chemistry 17(6), 2225-2235 (2009). 2.Bussenius, J.,Blazey, C.M.,Aay, N., et al. Discovery of XL888: A novel tropane-derived small molecule inhibitor of HSP90. Bioorganic & Medicinal Chemistry Letters 22(17), 5396-5404 (2012). 3.Lyman, S.K.,Crawley, S.C.,Gong, R., et al. High-content, high-throughput analysis of cell cycle perturbations induced by the HSP90 inhibitor XL888. PLoS One 6(3), 1-14 (2011). 4.Haarberg, H.E.,Paraiso, K.H.T.,Wood, E., et al. Inhibition of Wee1, AKT, and CDK4 underlies the efficacy of the HSP90 inhibitor XL888 in an in vivo model of NRAS-mutant melanoma. Molecular Cancer Therapeutics 12(6), 901-912 (2013). 5.Paraiso, K.H.T.,Haarberg, H.E.,Wood, E., et al. The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms. Clinical Cancer Research 18(9), 2502-2514 (2012). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 503.6 |
分子式 | C29H37N5O3 |
CAS号 | 1149705-71-4 |
稳定性 | ≥ 2 years |
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