aladdin 阿拉丁 A413769 Afuresertib (GSK2110183) 1047644-62-1 99%

中文名：Afuresertib (GSK2110183)

英文名：Afuresertib (GSK2110183)

纯度：Moligand™，≥99%

货号：A413769

Cas号：1047644-62-1

存储温度：避光,-20°C储存,充氩

运输条件：超低温运输

产品介绍：

Information

Afuresertib (GSK2110183) is a potent, orally bioavailableAktinhibitor withKiof 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Targets

Akt1 (Cell-free assay); Akt2 (Cell-free assay); Akt3 (Cell-free assay) 0.08 nM(Ki); 2 nM(Ki); 2.6 nM(Ki)

In vitro

Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.

In vivo

Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

Cell Research(from reference)

Cell lines：Hematological cell lines and solid tumor cell lines 

Concentrations：30 μM 

Incubation Time：72 h 

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