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GSK2110183 Sale

目录号 : GC33135

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

GSK2110183 Chemical Structure

Cas No.:1047634-63-8

规格 价格 库存 购买数量
2mg
¥2,082.00
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5mg
¥3,124.00
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10mg
¥4,463.00
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50mg
¥13,388.00
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100mg
¥18,743.00
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Sample solution is provided at 25 µL, 10mM.

Description

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

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.[1]

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.[1]

[1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.

化学性质

Cas No. 1047634-63-8 SDF
Canonical SMILES O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN
分子式 C18H16Cl2F2N4OS 分子量 445.31
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2456 mL 11.2281 mL 22.4563 mL
5 mM 0.4491 mL 2.2456 mL 4.4913 mL
10 mM 0.2246 mL 1.1228 mL 2.2456 mL
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