| 产品描述： | Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase. |
| 靶点： |
mTOR:1 nM (IC50);mTORC1;mTORC2;PI3Kα:219 nM (IC50);PI3Kβ:5.293 μM (IC50);PI3Kδ:230 nM (IC50);PI3Kγ:221 nM (IC50);Autophagy;PI3K;mTOR;Autophagy |
| 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 |
| 参考文献： |
1. Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55. 2. Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61. |
| 溶解性： |
DMSO : 55 mg/mL (177.80 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.233 ml |
16.164 ml |
32.328 ml |
| 5 mM |
0.647 ml |
3.233 ml |
6.466 ml |
| 10 mM |
0.323 ml |
1.616 ml |
3.233 ml |
| 50 mM |
0.065 ml |
0.323 ml |
0.647 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京