| 产品描述： | PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ). |
| 靶点： |
PI3Kα:2 nM (IC50);PI3Kα-H1047R:3 nM (IC50);PI3Kα-E545K:3 nM (IC50);PI3Kβ:7 nM (IC50);PI3Kδ:14 nM (IC50);PI3Kγ:16 nM (IC50);mTOR:3 nM (IC50);PI3K;mTOR |
| 体内研究： |
PKI-402 displays antitumor activity (i.v. route) in breast [MDA-MB-361: Her2+ and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models. PKI-402 causes regression in the MDA-MB-361 xenograft model. PKI-402 effect is most pronounced at 100 mg/kg (daily for 5 days, one round), which reduces initial tumor volume and prevents tumor re-growth for 70 days. In MDA-MB-361 tumor tissue, PKI-402 at 100 mg/kg (single dose) fully suppresses p-Akt at both the T308 and the S473 sites at 8 hours and induces cleaved PARP. At 24 hours, p-Akt suppression is still evident, as is cleaved PARP |
| 参考文献： |
1. Mallon R et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.752 ml |
8.762 ml |
17.524 ml |
| 5 mM |
0.35 ml |
1.752 ml |
3.505 ml |
| 10 mM |
0.175 ml |
0.876 ml |
1.752 ml |
| 50 mM |
0.035 ml |
0.175 ml |
0.35 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