S80890 |
PIK-90 |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)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.
- 靶點: 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
- 體內(nèi)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
- 參考文獻:
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.
- 溶解性: DMSO : 6.67 mg/mL (18.98 mM; ultrasonic and adjust pH to 2 with HCl)
- 保存條件: -20℃
- 配置溶液濃度參考:
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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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)