AMG 511

SKU: orb1218988

Description

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.

Key Properties

• CAS Number: 1253573-53-3
• MW: 517.58
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₈FN₉O₃S
• SMILES: C[C@H](c(cc1-c2nc(N)nc(C)n2)cnc1Nc(cc1F)cnc1OC)N(CC1)CCN1S(C)(=O)=O
• Target: PI3K
• Solubility: DMSO:33.33 mg/mL (64.40 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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).
• In Vitro:
  AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PI3K