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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Hazard and Precautionary Statements (GHS)

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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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AMG 511 Suppliers

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13913916777;
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
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15778
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Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7778
Advantage
56
Shanghai YuanQi Biotechnology Co., Ltd.
Tel
+86-2332782371 +86-18120098618
Email
sales@adobechem.com
Country
China
ProdList
1250
Advantage
50
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4796
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
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58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32470
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
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Changzhou Chenhong Biotechnology Co., Ltd.
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
4023
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58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
Energy Chemical
Tel
021-58432009 400-005-6266
Fax
021-58436166
Email
marketing1@energy-chemical.com
Country
China
ProdList
44893
Advantage
58

1253573-53-3, AMG 511Related Search:


  • AMG 511
  • AMG 511 (AMG-511
  • 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-
  • (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
  • 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
  • AMG 511, 10 mM in DMSO
  • 1253573-53-3
  • 253573-53-3
  • C22H28FN9O3S