貨號	規格	價格	上海	北京	武漢	南京
S81768-1mg	98%	￥240.00 S81768-1mg ￥240.00 現貨	10 10	-	-	-
S81768-5mg	98%	￥380.00 S81768-5mg ￥380.00 現貨	6 6	-	-	-
S81768-10mg	98%	￥610.00 S81768-10mg ￥610.00 現貨	6 6	-	-	-
S81768-25mg	98%	￥1070.00 S81768-25mg ￥1070.00 現貨	5 5	-	-	-

產品介紹

GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

產品描述：

GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

靶點：

PI3Kα:3.4 nM (IC50);PI3Kβ:12 nM (IC50);PI3Kδ:16 nM (IC50);PI3Kγ:16 nM (IC50);mTOR:30 nM (IC50);PI3K;?mTOR

體外研究：

GNE-493 is a low molecular weight, potent dual inhibitor of pan-PI3 kinases and mTOR. GNE-493 displays approximately equipotent inhibition of Class I PI3K isoforms, is submitted for screening in a 142 kinase panel provided by Invitrogen’s SelectScreen service. Of these kinases, only three are subject to greater than 50% inhibition by GNE-493, and none are inhibited greater than 80% when tested at 1 μM. Subsequently measured IC50s demonstrated that GNE-493 is more than 100-fold selective for PI3Kα over these three unrelated kinases (Aurora A IC50>10 μM, MLK1 IC50=591 nM and SYK IC50=371 nM)

體內研究：

To confirm and compare in vivo efficacy, GNE-493 is examined in the human MCF7.1 breast cancer xenograft model that harbors a PI3Kα activating mutation. Mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals. When achieving comparable levels of drug exposure, GNE-493 shows a similar suppression of the PI3K pathway and consequently, a similar efficacy profile against MCF7.1 breast tumors

參考文獻：

1. Sutherlin DP, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53(3):1086-97.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.685 ml	13.425 ml	26.85 ml
5 mM	0.537 ml	2.685 ml	5.37 ml
10 mM	0.268 ml	1.342 ml	2.685 ml
50 mM	0.054 ml	0.268 ml	0.537 ml

注意：

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

參考文獻

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GNE-493