1253573-53-3
1253573-53-3 structure
- Name: AMG 511
- Chemical Name: 1,3,5-Triazin-2-amine, 4-[2-[(5-fluoro-6-methoxy-3-pyridinyl)amino]-5-[(1R)-1-[4-(methylsulfonyl)-1-piperazinyl]ethyl]-3-pyridinyl]-6-methyl
- CAS Number: 1253573-53-3
- Molecular Formula: C22H28FN9O3S
- Molecular Weight: 517.58000
- Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
- Create Date: 2016-07-11 08:34:06
- Modify Date: 2024-01-19 18:09:56
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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].
| Name | 1,3,5-Triazin-2-amine, 4-[2-[(5-fluoro-6-methoxy-3-pyridinyl)amino]-5-[(1R)-1-[4-(methylsulfonyl)-1-piperazinyl]ethyl]-3-pyridinyl]-6-methyl |
|---|---|
| Synonyms | amg-511 |
| 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]. |
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| Related Catalog | |
| 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). |
| References |
| Molecular Formula | C22H28FN9O3S |
|---|---|
| Molecular Weight | 517.58000 |
| Exact Mass | 517.20200 |
| PSA | 160.73000 |
| LogP | 3.35950 |
| Hazard Codes | Xn |
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