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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
2 mg | $109 | In Stock | |
5 mg | $155 | In Stock | |
10 mg | Inquiry | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $299 | In Stock |
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]. |
Molecular Weight | 517.58 |
Formula | C22H28FN9O3S |
Cas No. | 1253573-53-3 |
Smiles | COc1ncc(Nc2ncc(cc2-c2nc(C)nc(N)n2)[C@H](C)N2CCN(CC2)S(C)(=O)=O)cc1F |
Relative Density. | no data available |
Storage | Powder: -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
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