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AMG 511

🥰Excellent
Catalog No. T14214Cas No. 1253573-53-3

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).

AMG 511

AMG 511

🥰Excellent
Catalog No. T14214Cas No. 1253573-53-3
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).
Pack SizePriceAvailabilityQuantity
1 mg$84In Stock
2 mg$109In Stock
5 mg$155In Stock
10 mgInquiryIn Stock
50 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$299In Stock
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Purity:≥98%
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Product Introduction

Bioactivity
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), 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).
Targets&IC50
PI3Kβ:6 nM (ki), PI3Kα:4 nM (ki), PI3Kγ:1 nM (ki), PI3Kδ:2 nM (ki)
In vitro
AMG 511 inhibits AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1].
In vivo
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].
Chemical Properties
Molecular Weight517.58
FormulaC22H28FN9O3S
Cas No.1253573-53-3
SmilesCOc1ncc(Nc2ncc(cc2-c2nc(C)nc(N)n2)[C@H](C)N2CCN(CC2)S(C)(=O)=O)cc1F
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 33.33 mg/mL (64.40 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9321 mL9.6603 mL19.3207 mL96.6034 mL
5 mM0.3864 mL1.9321 mL3.8641 mL19.3207 mL
10 mM0.1932 mL0.9660 mL1.9321 mL9.6603 mL
20 mM0.0966 mL0.4830 mL0.9660 mL4.8302 mL
50 mM0.0386 mL0.1932 mL0.3864 mL1.9321 mL

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