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

AMG 511 

Cat. No.: HY-13440 Purity: 98.81%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 251 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
25 mg USD 940 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9321 mL 9.6603 mL 19.3207 mL
5 mM 0.3864 mL 1.9321 mL 3.8641 mL
10 mM 0.1932 mL 0.9660 mL 1.9321 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References

Purity: 98.81%

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Keywords:

AMG 511AMG511AMG-511PI3KPhosphoinositide 3-kinaseglioblastomaPI3KαPI3KβPI3KδPI3KγmalignantgliomaInhibitorinhibitorinhibit

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AMG 511
Cat. No.:
HY-13440
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