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產品描述： 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). |
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靶點：
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 |
體內研究：
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 |
參考文獻：
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. |
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溶解性：
Soluble in DMSO |
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保存條件：
-20℃ |
配置溶液濃度參考：
|
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 |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京