Ganetespib

• CAT Number: I013970
• CAS Number: 888216-25-9
• Molecular Formula: C₂₀H₂₀N₄O₃
• Molecular Weight: 364.4
• Purity: ≥95%
• Target: HSP
• Solubility: DMSO: ≥ 32 mg/mL
• IUPAC Name: (5E)-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-(1-methylindol-5-yl)-1,2,4-triazolidin-3-one
• InChI: InChI=1S/C20H20N4O3/c1-11(2)14-9-15(18(26)10-17(14)25)19-21-22-20(27)24(19)13-4-5-16-12(8-13)6-7-23(16)3/h4-11,21,25H,1-3H3,(H,22,27)/b19-15-
• InChIKey: MWTUOSWPJOUADP-CYVLTUHYSA-N
• SMILES: CC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O

Ganetespib is a unique non-geldanamycin heat shock protein 90 (HSP90) inhibitor, with IC50 of 4 nM in OSA 8 cells.

Reference

[1]. Shimamura T, et al. Ganetespib (STA-9090), a Non-Geldanamycin HSP90 Inhibitor, has Potent Antitumor Activity in In Vitro and In Vivo Models of Non-Small Cell Lung Cancer. Clin Cancer Res. 2012 Jul 17.[2]. Ying W, et al. Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther. 2012 Feb;11(2):475-84.[3]. London CA, et al. Phase I evaluation of STA-1474, a prodrug of the novel HSP90 inhibitor ganetespib, in dogs with spontaneous cancer.PLoS One. 2011;6(11):e27018.[4]. Proia DA, et al. Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090) in cancer cells with activated JAK/STAT signaling. PLoS One. 2011 Apr 14;6(4):e18552.