S80689 |
PIK-75 |
源叶(MedMol) | 99% |
- 提示:详情请下载说明书。
- 产品描述: PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis
- 靶点: DNA-PK:2 nM (IC50);p110α:5.8 nM (IC50);p110γ:76 nM (IC50);p110δ:510 nM (IC50);p110β:1.3 μM (IC50);hsVPS34:2.6 μM (IC50);PI3KC2β:1 μM (IC50);PI3KC2α:10 μM (IC50);mTORC1:1 μM (IC50);mTORC2:10 μM (IC50);ATM:2.3 μM (IC50);ATR:21 μM (IC50);PI4KIIIβ:50 μM (IC50);Apoptosis;DNA-PK;PI3K
- 体内研究:
PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice
- 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. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. 3. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69. 4. Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15(17):5837-5844.
- 溶解性: DMSO : 11 mg/mL (22.51 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.046 ml 10.23 ml 20.461 ml 5 mM 0.409 ml 2.046 ml 4.092 ml 10 mM 0.205 ml 1.023 ml 2.046 ml 50 mM 0.041 ml 0.205 ml 0.409 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)