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Ganetespib(STA-9090)

  Cat. No.:  DC7320   Featured
Chemical Structure
888216-25-9
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Field of application
Ganetespib(STA-9090) is a unique triazolone-containing Hsp90 inhibitor with an IC50 of 4 nM in OSA 8 cells.
Cas No.: 888216-25-9
Chemical Name: Ganetespib
Synonyms: 3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy-4H-1,2,4-triazole;Ganetespib;5-[2,4-Dihydroxy-5-(1-methylethyl)phenyl]-2,4-dihydro-4-(1-methyl-1H-indol-5-yl)-3H-1,2,4-triazol-3-one;Ganetespib (STA-9090);(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;3H-1,2,4-Triazol-3-one, 5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-2,4-dihydro-4-(1-methyl-1H-i...;3H-1,2,4-Triazol-3-one, 5-[2,4-dihydroxy-5-(1-methylethyl)phenyl]-2,4-dihydro-4-(1-methyl-1H-indol-5-yl)-;STA 9090;STA-9090;STA9090;AK173506;2E8412Y946;3-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(1-methyl-indol-5-yl)-5-hydroxy-[1,2,4]triazole;5;5-[2,4-Dihydroxy-5-(1-methylethyl)phenyl]-2,4-dihydro-4-(1-methyl-1H-indol-5-yl)-3H-1,2,4-triazol-3-one (ACI);3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methylindol-5-yl)-5-hydroxy[1,2,4]triazole;ADX 1612
SMILES: O=C1N(C2C=C3C=CN(C3=CC=2)C)C(C2C(O)=CC(O)=C(C(C)C)C=2)=NN1
Formula: C20H20N4O3
M.Wt: 364.397804260254
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
In Vivo: Ganetespib (125 mg/kg, i.v.) accumulates in tumors relative to normal tissues and displays greater in vivo efficacy than 17-AAG without increased toxicity and inhibits proliferation and induces apoptosis in parallel with EGFR depletion in NCI-H1975 xenografts[1]. Ganetespib (100, 125, 150 mg/kg, i.v.) shows potent antitumor efficacy in solid and hematologic xenograft models of oncogene addiction, as evidenced by significant growth inhibition and/or regressions[2].
In Vitro: Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 values ranging 2-30 nM in genomically-defined NSCLC cell lines. Ganetespib is also approximately 20-fold more potent in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants[1]. Ganetespib exhibits potent in vitro cytotoxicity in a range of solid and hematologic tumor cell lines, induces the degradation of known Hsp90 client proteins, displays superior potency to the ansamycin inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG)[2]. Ganetespib is a potent HSP90 inhibitor, and shown to kill canine tumor cell lines in vitro[3]. Ganetespib possesses superior JAK/STAT inhibitory activity to both P6 and 17-AAG in terms of potency or duration of response in the HEL92.1.7 cells[4].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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