Afuresertib

产品编号: DC8411 Featured
Afuresertib
结构式
1047644-62-1
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中国地区超过5000个高品质化合物库存
应用领域
Afuresertib (GSK2110183) 是一个口服有效的,ATP 竞争性的选择性 pan-Akt 抑制剂,作用于 Akt1/Akt2/Akt3,Ki 值分别为 0.08/2/2.6 nM。
Cas No.: 1047644-62-1
名称: N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide
别名:
SMILES: CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)N[C@@H](CC3=CC(=CC=C3)F)CN)Cl
分子式: C18H17Cl2FN4Os
分子量: 427.32
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.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. For the detailed information of Afuresertib (GSK2110183), the solubility of Afuresertib (GSK2110183) in water, the solubility of Afuresertib (GSK2110183) in DMSO, the solubility of Afuresertib (GSK2110183) in PBS buffer, the animal experiment (test) of Afuresertib (GSK2110183), the cell expriment (test) of Afuresertib (GSK2110183), the in vivo, in vitro and clinical trial test of Afuresertib (GSK2110183), the EC50, IC50,and affinity,of Afuresertib (GSK2110183), For the detailed information of Afuresertib (GSK2110183), the solubility of Afuresertib (GSK2110183) in water, the solubility of Afuresertib (GSK2110183) in DMSO, the solubility of Afuresertib (GSK2110183) in PBS buffer, the animal experiment (test) of Afuresertib (GSK2110183), the cell expriment (test) of Afuresertib (GSK2110183), the in vivo, in vitro and clinical trial test of Afuresertib (GSK2110183), the EC50, IC50,and affinity,of Afuresertib (GSK2110183), Please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC8411 Afuresertib Afuresertib (GSK2110183) 是一个口服有效的,ATP 竞争性的选择性 pan-Akt 抑制剂,作用于 Akt1/Akt2/Akt3,Ki 值分别为 0.08/2/2.6 nM。
DC7994 Afuresertib HCl Afuresertib hydrochloride (GSK 2110183 hydrochloride) 是一个口服有效的,ATP 竞争性的选择性 pan-Akt 抑制剂,作用于 Akt1/Akt2/Akt3,Ki 值分别为 0.08/2/2.6 nM。