17-AAG

17-AAG is an inhibitor of heat shock protein 90 (Hsp90) and a derivative of geldanamycin (Item No. 13355) that selectively inhibits BT474 tumor cell Hsp90 over fibroblast Hsp90 (IC₅₀s = 5 and 943 nM, respectively).¹ It inhibits the growth of prostate cancer cell lines (IC₅₀s = 25-45 nM) and promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC₅₀s = 4-72 nM).^2,3 In vivo, 17-AAG (25 mg/kg, i.p.) reduces tumor size in a G-415 gallbladder cancer mouse xenograft model.⁴

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1. Kamal, A., Thao, L., Sensintaffar, J., et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature 425(6956), 407-410 (2003).

2. Solit, D.B., Zheng, F.F., Drobnjak, M., et al. 17-allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clin. Cancer Res. 8(5), 986-993 (2002).

3. Münster, P.N., Marchion, D.C., Basso, A.D., et al. Degredation of HER2 by ansamycins induces growth arrest and apoptosis in cells with HER2 overexpression via a HER3, phosphatidylinositol 3'-kinase-AKT-dependent pathway. Cancer Res. 62(11), 3132-3137 (2002).

4. Weber, H., Valbuena, J.R., Barbhuiya, M.A., et al. Small molecule inhibitor screening identifified HSP90 inhibitor 17-AAG as potential therapeutic agent for gallbladder cancer. Oncotarget 8(16), 26169-26184 (2017).