貨號	規(guī)格	價格	上海	北京	武漢	南京
S81822-5mg	≥96%	￥930.00 S81822-5mg ￥930.00 2-3天	0 貨期：2-3天	-	-	-
S81822-10mg	≥96%	￥1400.00 S81822-10mg ￥1400.00 2-3天	0 貨期：2-3天	-	-	-
S81822-50mg	≥96%	￥3900.00 S81822-50mg ￥3900.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively

產(chǎn)品描述：

靶點：

Akt1:0.08 nM (Ki);Akt2:2 nM (Ki);Akt3;2.6 nM (Ki);Akt1 E17K mutant:0.2 nM (IC50);PKCη:210 nM (IC50);PKC-βI;430 nM (IC50);ROCK:100 nM (IC50);PKCθ:510 nM (IC50);ROCK;?Akt;?PKC

體外研究：

Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response

體內(nèi)研究：

Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts

參考文獻(xiàn)：

1. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. 2. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.156 ml	10.781 ml	21.562 ml
5 mM	0.431 ml	2.156 ml	4.312 ml
10 mM	0.216 ml	1.078 ml	2.156 ml
50 mM	0.043 ml	0.216 ml	0.431 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(xiàn)

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Afuresertib (hydrochloride)