Ganetespib (888216-25-9) is an inhibitor of heat shock protein 90 (IC50 = 19 nM, canine C2 malignant mast cells; 4 nM, canine BR malignant mast cells) binding to the N-terminal ATP site.1 It displayed potent cytotoxicity against a panel of 57 transformed cell lines of both hematologic and solid tumors with IC50’s between 14 and 280 nM.2 Ganetespib enhanced T-cell-mediated killing of human melanoma cells and potentiated responses to anti-CTLA4 and anti-PD1 therapy via upregulation of interferon response genes.3 In multiple clinical trials for various cancers.
References/Citations for Ganetespib
- Lin et al. (2008), The novel HSP90 inhibitor STA-9090 exhibits activity against Kit-dependent and -independent malignant mast cell tumors; Exp. Hematol. 36 1266
- Ying et al. (2012), Ganetespib, a Unique Triazoline-Containing Hsp90 Inhibitor, Exhibits Potent Antitumor Activity and a Superior Safety Profile for Cancer Therapy; Mol. Cancer Ther. 11 475
- Mbofung et al. (2017), HSP90 inhibition enhances cancer immunotherapy by upregulating interferon response genes; Nat. Commun. 8 451