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Ganetespib (STA-9090)

Non-geldanamycin Hsp90 inhibitor

Ganetespib (STA-9090)

Catalog No. A4385
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $190.00 In stock
10mg $259.00 In stock
50mg $754.00 In stock
200mg $1,742.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Biological Activity

Description Ganetespib (STA-9090) is an inhibitor of HSP90 with IC50 of 4 nM in OSA 8 cells.
Targets HSP90          
IC50 4 nM          

Ganetespib (STA-9090) Dilution Calculator

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Chemical Properties

Cas No. 888216-25-9 SDF Download SDF
Synonyms STA9090, STA 9090
Chemical Name (5Z)-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
Canonical SMILES CC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O
Formula C20H20N4O3 M.Wt 364.4
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Ganetespib (also known as STA-9090), 5-[2,4-dihydroxy-5-(1 methylethyl)phenyl]-2,4 dihydro-4-(1-methyl-1H indol-5 yl)-3H-1,2,4 triazole-3-one, is a potent small-molecule inhibitor of heat shock protein 90 (Hsp90), which binds to the ATP pocket in the N-terminus of Hsp90 resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile. Results of previous studies indicate that ganetespib exhibits antitumor activity against a broad range of human cancers, including lung cancer, prostate cancer, colon cancer, breast cancer, melanoma and leukemia.

Reference

Weiwen Ying, Zhenjian Du, Lijun Sun, Kevin P. Foley, David A. Proia, Ronald K. Blackman, Dan Zhou, Takayo Inoue, Noriaki Tatsuta, Jim Sang, Shuxia Ye, Jamie Acquaviva, Luisa Shin Ogawa, Yumiko Wada, James Barsoum, and Keizo Koya. Ganetespib, a unqiue triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther 2012; 11: 475-484

Jonathan W Goldman, Robert N Raju, Gregory A Gordon, Iman El-Hariry, Florentina Teofilivivi, Vojo M Vukovic, Robert Bradley, Michael D Karol, Yu Chen, Wei Guo, Takayo Inoue and Lee Rosen. A first in human, safety, pharmacokinetics, and clinical activity phase I study of once weekly administration of the Hsp90 inhibitor ganetespib (STA-9090) in patients with solid malignancies. BMC Cancer 2013; 13:152