| Identification | Back Directory | [Name]
AMG 511 | [CAS]
1253573-53-3 | [Synonyms]
AMG 511
AMG 511
(AMG-511
AMG511,AMG-511,Inhibitor,PI3K,PI3Kβ,AMG 511,malignant,PI3Kγ,PI3Kα,Phosphoinositide 3-kinase,inhibit,glioblastoma,PI3Kδ,glioma
(R)-4-(2-((5-Fluoro-6-methoxypyridin-3-yl)amino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine
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- | [Molecular Formula]
C22H28FN9O3S | [MOL File]
1253573-53-3.mol | [Molecular Weight]
517.58 |
| Chemical Properties | Back Directory | [solubility ]
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
AMG-511 is a PI3Kα inhibitor used as a cancer therapeutic due to its effect on cell growth and cell survival. | [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). |
| [IC 50]
PI3Kα: 4 nM (Ki); PI3Kβ: 6 nM (Ki); PI3Kδ: 2 nM (Ki); PI3Kγ: 1 nM (Ki) | [References]
[1] MARK H. NORMAN*. Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511[J]. Journal of Medicinal Chemistry, 2012, 55 17: 7796-7816. DOI: 10.1021/jm300846z |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|