- 英文名称
- Ganetespib
- 分子式
- C20H20N4O3
- 分子量
- 364.4
- 中文别名
- Ganetespib; 3-(2,4-二羟基-5-异丙基苯基)-4-(1-甲基吲哚-5-基)-5-羟基-4H-1,2,4-三氮唑; 3-(2,4-二羟基-5-异丙基苯基)-4-(1-甲基吲哚-5-基)-5-羟基-4H-1,2,4-三唑; 3-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-1H-1,2,4-triazol-5(4H)-one; STA-9090; STA9090; 5-(2,4-Dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2,4-dihydro-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)-3H-1,2,4-triazol-3-one; 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)-; 5-(2,4-dihydroxy-5-isopropylphenyl)-4-(1-methyl-1H-indol-5-yl)-2H-1,2,4-triazol-3(4H)-one
- 用途
- HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡而不影响正常成骨细胞；是STA-1474的活性代谢物，处于Phase 3阶段；对恶性肥大细胞系的IC50比17-AAG低10-15倍；抑制MG63细胞系IC50为43 nM；结合Hsp90的N末端ATP结合域，引起多重致瘤性Hsp90受体蛋白降解；纳摩尔级低浓度下有效阻滞细胞增殖并诱导广泛人肿瘤细胞系凋亡，对受体酪氨酸激酶抑制剂和tanespimycin耐受的细胞系也有作用；给药导致小鼠体内肿瘤显著缩减且毒性较低，肿瘤渗透性优于tanespimycin；在恶性肥大细胞和OSA异种移植模型中抑制体内肿瘤生长，25 mg/kg/day给药3天重复两个周期%T/C值为18，耐受性良好
