貨號	規(guī)格	價格	上海	北京	武漢	南京
S83856-1mg	≥99%	￥800.00 S83856-1mg ￥800.00 2-3天	0 貨期：2-3天	-	-	-
S83856-5mg	≥99%	￥1600.00 S83856-5mg ￥1600.00 2-3天	0 貨期：2-3天	-	-	-
S83856-10mg	≥99%	￥2600.00 S83856-10mg ￥2600.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

產(chǎn)品描述：

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

靶點：

PI3Kα:2 nM (IC50);PI3Kβ:9.4 nM (IC50);PI3Kδ:14 nM (IC50);PI3Kγ:2.7 nM (IC50);mTOR:5.4 nM (IC50);PI3K;?mTOR

體外研究：

NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines

體內(nèi)研究：

In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight

參考文獻：

1. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.593 ml	7.966 ml	15.932 ml
5 mM	0.319 ml	1.593 ml	3.186 ml
10 mM	0.159 ml	0.797 ml	1.593 ml
50 mM	0.032 ml	0.159 ml	0.319 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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