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Chemical Structure : STA-9090
CAS No.: 888216-25-9
Catalog No.: PC-20710Not For Human Use, Lab Use Only.
Ganetespib (STA 9090) is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 100 mg | $488 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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Ganetespib (STA 9090) is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
Ganetespib blocks the ability of HSP90 to bind to biotinylated geldanamycin and disrupts the association of HSP90 with its cochaperone, p23, more potently than 17-AAG.
Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 of 2-30 nM, in NSCLC cell lines.
Ganetespib is also approximately 20-fold more potent than 17-AAG in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants.
Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and acts as a potent Hsp90 inhibitor by inducing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2, c-Met, and Wilms' tumor 1.
| M.Wt | 364.41 | |
| Formula | C20H20N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
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1. Lin TY, et al. Exp Hematol. 2008 Oct;36(10):1266-77.
2. McCleese JK, et al. Int J Cancer. 2009 Dec 15;125(12):2792-801.
3. Bansal H, et al. Blood. 2010 Nov 25;116(22):4591-9.
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