AMG 511CAS号: 1253573-53-3分子式: C22H28FN9O3S分子量: 517.58描述储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks(Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively). It exhibits anti-tumor activity in mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease.
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储存/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.
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基本信息 | |
可溶性/溶解性 |
DMSO:33.33 mg/mL (64.40 mM)
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生物活性 | |
靶点 |
PI3Kδ:2 nM (ki), PI3Kα:4 nM (ki), PI3Kβ:6 nM (ki), PI3Kγ:1 nM (ki)
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In vitro(体外研究) |
AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1].
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In vivo(体内研究) |
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile[1]. AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.). And it inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days)[1].
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