MPC-3100

MPC-3100 is an inhibitor of heat shock protein 90 (Hsp90; IC₅₀ = 0.14 µM in a fluorescence polarization assay).¹ It inhibits proliferation of a variety of cancer cell lines, including colon, prostate, ovarian, gastric, and breast cancer cells (IC₅₀s = 0.2-0.55 µM), as well as MV4-11 leukemia, A549 non-small cell lung cancer (NSCLC), NCI H69 SCLC, and multidrug-resistant NCI/ADR-RES cells (IC₅₀s = 0.25, 0.77, 0.15, and 4.3 µM, respectively). MPC-3100 induces degradation of the Hsp90 client proteins Akt and HER2 (IC₅₀s = 0.1-0.5 µM) and a compensatory Hsp70 response in NCI N87, HCT116, and DU145 cell lysates. It also induces Hsp70 expression in the liver and tumor tissue and reduces tumor growth in an NCI N87 mouse xenograft model when administered at doses of 50 and 75 mg/kg. It induces tumor regression in the same model when administered at doses of 125 and 200 mg/kg.

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1. Kim, S.H., Bajji, A., Tangallapally, R., et al. Discovery of (2S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]-9H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor. J. Med. Chem. 55(17), 7480-7501 (2012).