货号	规格	价格	上海	北京	珠海	重庆	武汉
S80689-5mg买3赠1	99.10%	￥200.00 S80689-5mg ￥200.00 现货（买3赠1）	3 3	-	-	-	-
S80689-10mg买3赠1	99.10%	￥320.00 S80689-10mg ￥320.00 现货（买3赠1）	7 7	-	-	-	-
S80689-25mg买3赠1	99.10%	￥760.00 S80689-25mg ￥760.00 现货（买3赠1）	5 5	-	-	-	-
S80689-50mg买3赠1	≥99%	￥1280.00 S80689-50mg ￥1280.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S80689-100mg买3赠1	≥99%	￥1920.00 S80689-100mg ￥1920.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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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

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。

参考文献

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