Ganetespib blocked the ability of HSP90 to bind to biotinylated geldanamycin and disrupted the association of HSP90 with its cochaperone, p23, more potently than 17-AAG. In genomically defined NSCLC cell lines, ganetespib caused depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC(50) values ranging 2 to 30 nmol/L, substantially lower than those required for 17-AAG (20-3,500 nmol/L). Ganetespib was also approximately 20-fold more potent in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants.
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名称 | Ganetespib(STA-9090) |
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Iupac 化学名称 | 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one |
同义词 | Ganetespib,STA-9090,STA9090,STA 9090 |
英文同义词 | Ganetespib,STA-9090,STA9090,STA 9090 |
分子式 | C20H20N4O3 |
分子量 | 364.4 |
Smile | OC1=C(C=C(C(=C1)O)C(C)C)C=1N(C(NN1)=O)C=1C=C2C=CN(C2=CC1)C |
InChiKey | RVAQIUULWULRNW-UHFFFAOYSA-N |
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/h4-11,25-26H,1-3H3,(H,22,27) |
Cas号 | 888216-25-9 |
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