ChemicalBook > CAS DataBase List > AMG 511
AMG 511
- Product Name
- AMG 511
- CAS No.
- 1253573-53-3
- Chemical Name
- AMG 511
- Synonyms
- AMG 511;AMG 511 (AMG-511;AMG 511, 10 mM in DMSO;AMG511,AMG-511,Inhibitor,PI3K,PI3Kβ,AMG 511,malignant,PI3Kγ,PI3Kα,Phosphoinositide 3-kinase,inhibit,glioblastoma,PI3Kδ,glioma;4-{2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[(1R)-1-(4-methanesulfonylpiperazin-1-yl)ethyl]pyridin-3-yl}-6-methyl-1,3,5-triazin-2-amine;(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-
- CBNumber
- CB32666818
- Molecular Formula
- C22H28FN9O3S
- Formula Weight
- 517.58
- MOL File
- 1253573-53-3.mol
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AMG 511 Property
- solubility
- Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml - form
- Solid
- color
- Light yellow to yellow
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N-Bromosuccinimide Price
TRC
- Product number
- A576580
- Product name
- AMG-511
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0006892
- Product name
- AMG511
- Purity
- 98.81%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0006892
- Product name
- AMG511
- Purity
- 98.81%
- Packaging
- 10mg
- Price
- $420
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-0006892
- Product name
- AMG511
- Purity
- 98.81%
- Packaging
- 25mg
- Price
- $940
- Updated
- 2021/12/16
AK Scientific
- Product number
- SYN5398
- Product name
- AMG-511
- Packaging
- 100mg
- Price
- $2680
- Updated
- 2021/12/16
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AMG 511 Chemical Properties,Usage,Production
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
AMG 511 Preparation Products And Raw materials
Raw materials
Preparation Products
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