
簡要描述:GSK2110183 1047644-62-1GSK2110183 is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).
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| 品牌 | absin | CAS | 1047644-62-1 |
|---|---|---|---|
| 分子式 | C18H17Cl2FN4OS | 純度 | 98% |
| 分子量 | 427.32 | 貨號 | abs47027863 |
| 規(guī)格 | 2mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent pan-AKT inhibitor | 應用領域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
GSK2110183 1047644-62-1
| 產(chǎn)品描述 | |
| 描述 | GSK2110183 is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM). |
| 純度 | 98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | Afuresertib;GSK-2110183C |
| 可溶性/溶解性 | DMSO : ≥ 40 mg/mL (93.61 mM) |
| 生物活性 | |
| 靶點 | Akt1,Akt2,Akt3 |
| In vitro(體外研究) | 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 |
| In vivo(體內(nèi)研究) | 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. |
| 研究領域 | |
| 研究領域 | CancerCell DeathApoptosisMetabolism CancerSignal transductionProtein phosphorylationSerine/threonine kinasesAKT EpigeneticsCell cycleApoptosisNuclear MetabolismPathways and ProcessesMetabolism processesApoptosis Signal TransductionProtein PhosphorylationSer / Thr KinasesPKB / AKT Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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