货号	规格	价格	上海	北京	珠海	重庆	武汉
S80011-1mg买3赠1	99.30%	￥236.00 S80011-1mg ￥236.00 现货（买3赠1）	5 5	-	-	-	-
S80011-5mg促销	99.30%	￥345.00 ￥344.00 S80011-5mg ￥344.00 现货	5 5	-	-	-	-
S80011-10mg买3赠1	99.30%	￥550.00 S80011-10mg ￥550.00 现货（买3赠1）	5 5	-	-	-	-
S80011-25mg买3赠1	99.30%	￥868.00 S80011-25mg ￥868.00 现货（买3赠1）	6 0 6	-	-	-	-
S80011-50mg	99.30%	￥1380.00 S80011-50mg ￥1380.00 现货	5 5	-	-	-	-
S80011-100mg	≥97%	￥2220.00 S80011-100mg ￥2220.00 现货	2 2	-	-	-	-

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产品描述：

Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.

靶点：

PI3Kα:14 nM (IC50);PI3Kα-H1047R:5.6 nM (IC50);PI3Kα-E545K:6.7 nM (IC50);PI3Kα-E542K:6.7 nM (IC50);PI3Kγ:36 nM (IC50);PI3Kβ:120 nM (IC50);PI3Kδ:500 nM (IC50);PI3KC2β:5.3 μM (IC50);mTOR:1.6 μM (IC50);PI3K;mTOR

体内研究：

Mice bearing BT-474 tumors (n=14) are orally administered 50 mg/kg of Everolimus on a daily basis for 31 days and then randomized. After randomization, the mice are orally administered 50 mg/kg of Everolimus (n=4) and 12.5 mg/kg (n=5), and 25 mg/kg (n=5) of Izorlisib on a daily basis for 7 days. C, the vehicle-, Everolimus, and CH5132799-treated (25 mg/kg) tumors are resected at 4 hours after terminal administration in B, lysed, and analyzed by Western blotting. Izorlisib administration leads to a remarkable regression in a dose-dependent manner of the tumors regrown after the long-term Everolimus treatment. The tumors are resected at the end of treatment and analyzed by Western blotting with respect to PI3K pathway inhibition. Izorlisib suppresses various effectors in the PI3K pathway, including Akt, FoxO1, S6K, S6, and 4E-BP1, whereas Everolimus inhibits only phosphorylation of S6K and S6, both downstream effectors of mTORC1

参考文献：

1. Tanaka H, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res, 2011, 17(10), 3272-3281. 2. Ohwada J, et al. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Leff, 2011, 21(6), 1767-1772.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.65 ml	13.248 ml	26.496 ml
5 mM	0.53 ml	2.65 ml	5.299 ml
10 mM	0.265 ml	1.325 ml	2.65 ml
50 mM	0.053 ml	0.265 ml	0.53 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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