貨號	規(guī)格	價格	上海	北京	武漢	南京
S80011-1mg	≥97%	￥236.00 S80011-1mg ￥236.00 現(xiàn)貨	5 5	-	-	-
S80011-5mg	≥97%	￥344.00 S80011-5mg ￥344.00 現(xiàn)貨	5 5	-	-	-
S80011-10mg	≥97%	￥550.00 S80011-10mg ￥550.00 現(xiàn)貨	5 5	-	-	-
S80011-25mg	≥97%	￥868.00 S80011-25mg ￥868.00 現(xiàn)貨	6 6	-	-	-
S80011-50mg	≥97%	￥1389.00 S80011-50mg ￥1389.00 現(xiàn)貨	5 5	-	-	-
S80011-100mg	≥97%	￥2222.00 S80011-100mg ￥2222.00 現(xiàn)貨	3 3	-	-	-

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產(chǎn)品介紹

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

產(chǎn)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.

靶點：

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

體內(nèi)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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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