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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.

• 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.

• 溶解性： DMSO  :  6.67  mg/mL  (18.98  mM;  ultrasonic  and  adjust  pH  to  2  with  HCl)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	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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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *