产品
编 号：F095974
分子式：C22H28FN9O3S
分子量：517.58
分子式：C22H28FN9O3S
分子量：517.58
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1253573-53-3
产品详情
生物活性：
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
体内研究：
AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days).AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile.Animal Model:Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model
Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:Oral administration, daily, for 12 days
Result:Inhibited tumor growth.
Animal Model:Male Sprague-Dawley rats
Dosage:1 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).
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.
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
体内研究：
AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days).AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile.Animal Model:Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model
Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:Oral administration, daily, for 12 days
Result:Inhibited tumor growth.
Animal Model:Male Sprague-Dawley rats
Dosage:1 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).
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.
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