1. PI3K/Akt/mTOR
  2. PI3K
  3. AMG 511

AMG 511 

Cat. No.: HY-13440
Handling Instructions

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.

For research use only. We do not sell to patients.

AMG 511 Chemical Structure

AMG 511 Chemical Structure

CAS No. : 1253573-53-3

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Description

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[1].

IC50 & Target

PI3Kα

4 nM (Ki)

PI3Kβ

6 nM (Ki)

PI3Kδ

2 nM (Ki)

PI3Kγ

1 nM (Ki)

In Vitro

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1].

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)[1].
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile[1].

Animal Model: Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model[1]
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[1]
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).
Molecular Weight

517.58

Formula

C₂₂H₂₈FN₉O₃S

CAS No.

1253573-53-3

SMILES

NC1=NC(C2=CC([[email protected]](N3CCN(S(=O)(C)=O)CC3)C)=CN=C2NC4=CC(F)=C(OC)N=C4)=NC(C)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

AMG 511AMG511AMG-511PI3KPhosphoinositide 3-kinaseglioblastomaPI3KαPI3KβPI3KδPI3KγmalignantgliomaInhibitorinhibitorinhibit

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