帕他色替双盐酸盐
| CAS号 | 1396257-94-5 | 货号 | BCP23821 |
| 中文名 | 帕他色替双盐酸盐 | ||
| 英文名 | Ipatasertib dihydrochloride | ||
| 中文别名 | 双盐酸帕他色替; | ||
| 英文别名 | GDC0068 2HCl;Ipatasertib 2HCl;GDC0068 dihydrochloride;GDC-0068 dihydrochloride; RG-7440 dihydrochloride; | ||
| 分子式 | C24H34Cl3N5O2 | 分子量 | 530.92 |
| 生物活性 | Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with Docetaxel induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with Carboplatin. The combination of Ipatasertib with Docetaxel or Carboplatin is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone. | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | AKT | ||
结构式
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