KU-0063794   938440-64-3

 INK 128 (MLN0128)
分子式：C15H15N7O  分子量：309.33
 
產(chǎn)品描述
INK 128是有效的，選擇性mTOR抑制劑，IC50為1 nM;對I型PI3K亞型的作用效果低200倍以上,與Rapamycin相比，優(yōu)先抑制mTORC1/2，且對促侵襲基因敏感。
靶點
mTOR
         
IC50
1 nM
         
體外研究
INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases.As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors.
體內研究
In a ZR-75-1 breast cancer xenograft model, INK 128 shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day.Daily, oral administration of INK 128 inhibits angiogenesis and tumor growth in multiplexenograft models.
溶解性
DMSO 62 mg/mL，水 <1 mg/mL，乙醇 2 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO