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Afuresertib (hydrochloride) Sale

(Synonyms: GSK2110183 hydrochloride) 目录号 : GC42747

A pan-Akt inhibitor

Afuresertib (hydrochloride) Chemical Structure

Cas No.:1047645-82-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥785.00
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2mg
¥560.00
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5mg
¥770.00
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10mg
¥1,155.00
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50mg
¥3,640.00
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100mg
¥5,530.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

MPM cells are seeded in 96-well plates (cell density, 2.5×103 cells/well) and are incubated for 24 h at 37°C. Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g., Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer[1].

References:

[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

产品描述

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[1][2].

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[1].

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[2].

References:
[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

Chemical Properties

Cas No. 1047645-82-8 SDF
别名 GSK2110183 hydrochloride
Canonical SMILES FC1=CC=CC(C[C@@H](CN)NC(C2=CC(C3=C(Cl)C=NN3C)=C(Cl)S2)=O)=C1.Cl
分子式 C18H17Cl2FN4OS•HCl 分子量 463.8
溶解度 DMF: 50 mg/mL,DMSO: 30 mg/mL,Ethanol: 50 mg/mL,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL 储存条件 Store at -20°C, protect from light, stored under nitrogen
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1561 mL 10.7805 mL 21.561 mL
5 mM 0.4312 mL 2.1561 mL 4.3122 mL
10 mM 0.2156 mL 1.0781 mL 2.1561 mL
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