名称 | AMG 511 |
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), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473). |
体外活性 | AMG 511 inhibits AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1]. |
体内活性 | 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]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 33.33 mg/mL (64.40 mM), Sonication is recommended.
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关键字 | AMG-511 | Inhibitor | AMG511 | PI3K | PI3Kβ | malignant | PI3Kγ | PI3Kα | Phosphoinositide 3-kinase | inhibit | glioblastoma | PI3Kδ | glioma | AMG 511 |
相关产品 | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | GDC0084 | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
相关库 | 抗胰腺癌化合物库 | 经典已知活性库 | 激酶抑制剂库 | 抗乳腺癌化合物库 | 抗肥胖化合物库 | 抗氧化化合物库 | 血管生成库 | 代谢化合物库 | 抗衰老化合物库 | 已知活性化合物库 |