Sapanisertib (MLN0128, INK 128, TAK-228) 是一种有效的，选择性mTOR抑制剂，在无细胞试验中IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。Phase 1。
| CAS No. | 1224844-38-5 |
| 生物活性 | Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase. |
| 分子式 | C15H15N7O |
| 分子量 | 309.33 |
| 储存条件 | Powder -20℃ 3 years |
| 溶解性数据 | DMSO : 55 mg/mL (177.80 mM; Need ultrasonic) |
| 体内研究 | In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) shows tumor growth inhibition efficacy at a dose of 0.3 mg/kg/day. 4EBP1 and p70S6K1/2 phosphorylation is completely restored to wild-type levels after treatment with INK128 in PtenL/L mice. Sapanisertib (INK-128) treatment results in a 50% decrease in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and induces programmed cell death in multiple cancer cell lines in mice. |
| 体外研究 | Sapanisertib (INK-128) exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases. Sapanisertib (INK-128) selectively decreases the expression of YB1, MTA1, vimentin and CD44 at the protein but not transcript level in PC3 cells. Sapanisertib (INK-128) decreases the invasive potential of PC3 prostate cancer cells. Furthermore, Sapanisertib (INK-128) inhibits cancer cell migration starting at 6 h of treatment, precisely correlating with when decreases in the expression of pro-invasion genes are evident, but preceding any changes in the cell cycle or overall global protein synthesis. |
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| 纯度及产品资料 | 98% |
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