In vitro
AT13387 is a novel, high-affinity, and non-geldanamycin inhibitor of the molecular chaperone Hsp90(heat-shock protein 90) by fragment based drug design. AT13387 can potently inhibit Hsp90 with IC50 of 18 nM in A375 cells. In vitro, AT13387 shows activity against a wide array of tumor cell lines, including lung cancer cell lines. AT13387 showed a median EC50 value of 41 nM against the PPTP and exhibited activity consistent with a cytotoxic effect.AT13387 can induce the degradation of specific HSP90 client proteins for up to 7 days in tumor cell lines in vitro. AT13387 caninhibit the proliferation of imatinib-sensitive (GIST882, GIST-T1) and -resistant (GIST430, GIST48) cell lines, including those resistant to the geldanamycin analogue HSP90 inhibitor, 17-AAG.
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