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产品描述： PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively. |
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靶点：
p110α:11 nM (IC50);p110γ:18 nM (IC50);p110δ:58 nM (IC50);p110β:350 nM (IC50);hsVPS34:830 nM (IC50);PI3KC2β:64 nM (IC50);PI3KC2α:47 nM (IC50);DNA-PK:13 nM (IC50);ATM:610 nM (IC50);PI4KIIIα:830 nM (IC50);PI4KIIIβ:3.1 μM (IC50);mTORC1:1.05 μM (IC50);ATR:15 μM (IC50);DNA-PK;PI3K |
体内研究：
To test the efficacy of Roscovitine and PIK-90 in vivo, GBM43 cells are implanted s.c. into nude mice. Mice with established tumors are randomized into four treatment groups: vehicle (PBS:H2O), Roscovitine, PIK-90, or PIK-90 plus Roscovitine. After 12 d of treatment, both Roscovitine and PIK-90 show clear single-agent efficacy, with tumor size in mice treated with Roscovitine and PIK-90 in combination significantly smaller than either vehicle or monotherapy-treated controls. Roscovitine is less effective than PIK-90 in blocking proliferation (levels of Ki-67), whereas combination therapy shows essentially additive antiproliferative effects |
参考文献：
1. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. 2. Niedermeier M, et al. Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. Blood. 2009 May 28;113(22):5549-57. 3. Cheng CK, et al. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12722-7. |
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溶解性：
DMSO : 6.67 mg/mL (18.98 mM; ultrasonic and adjust pH to 2 with HCl) |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.846 ml |
14.23 ml |
28.461 ml |
| 5 mM |
0.569 ml |
2.846 ml |
5.692 ml |
| 10 mM |
0.285 ml |
1.423 ml |
2.846 ml |
| 50 mM |
0.057 ml |
0.285 ml |
0.569 ml |
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| 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
北京