| 产品描述： | NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα. |
| 靶点： |
PI3Kα:2 nM (IC50);PI3Kβ:9.4 nM (IC50);PI3Kδ:14 nM (IC50);PI3Kγ:2.7 nM (IC50);mTOR:5.4 nM (IC50);PI3K; mTOR |
| 体外研究： |
NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines |
| 体内研究： |
In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight |
| 参考文献： |
1. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.593 ml |
7.966 ml |
15.932 ml |
| 5 mM |
0.319 ml |
1.593 ml |
3.186 ml |
| 10 mM |
0.159 ml |
0.797 ml |
1.593 ml |
| 50 mM |
0.032 ml |
0.159 ml |
0.319 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