AMG 458
- CAS No.
- 913376-83-7
- Chemical Name:
- AMG 458
- Synonyms
- CS-530;AMG 458;AMG458/AMG-458;AMG 458 USP/EP/BP;AMG-458 AMG458 c-MET inhibitor;AMG458,inhibit,Inhibitor,c-Met/HGFR,AMG-458;1-(2-Hydroxy-2-methylpropyl)-N-[5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl]-5-methyl-3-oxo-2-;1-(2-Hydroxy-2-methylpropyl)-N-[5-[(7-methoxyquinolin-4-yl)oxy]pyridin-2-yl]-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide;1H-Pyrazole-4-carboxamide, 2,3-dihydro-1-(2-hydroxy-2-methylpropyl)-N-[5-[(7-methoxy-4-quinolinyl)oxy]-2-pyridinyl]-5-methyl-3-oxo-2-phenyl-
- CBNumber:
- CB62500951
- Molecular Formula:
- C30H29N5O5
- Molecular Weight:
- 539.58
- MOL File:
- 913376-83-7.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:13
AMG 458 Chemical Properties,Uses,Production
Enzyme inhibitor
This potent c-Met protein kinase inhibitor (FW = 539.58 g/mol; CAS 913376-83-7; Solubility: 21 mg/mL DMSO; ~1 mg/mL H2O), also named 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin- 2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide, targets the MET proto-oncogene product c-Met, which is the hepatocyte growth factor receptor possessing tyrosine-kinase activity. The primary single-chain precursor protein is posttranslationally cleaved to produce the a and b subunits that are disulfide linked to form the mature receptor. Various mutations in the MET gene are associated with papillary renal carcinoma. AMG-458 preferentially inhibits c-Met (Ki = 1.2 nM), showing ~350-fold greater potency than VEGFR2 in cells. AMG-458 significantly inhibited tumor growth in the NIH3T3/TPR-Met and U-87 MG xenograft models with no adverse effect on body weight. AMG 458 binds covalently to liver microsomal proteins from rats and humans, even in the absence of NADPH. When [14C]AMG-458 is incubated with liver microsomes in the presence of glutathione or N-acetyl cysteine, quinolone-type thioether adducts can be detected by radiochromatographyand LC/MS/MS analysis. AMG-458 was more effective in cells that expressed higher levels of c-Met/p-Met, suggesting that higher levels of c- Met and p-Met in non-small cell lung cancer (NSCLC) tissue may classify a subset of tumors that are more sensitive to molecular therapies against this receptor.
AMG 458 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 25247 | 58 | Inquiry |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
TargetMol Chemicals Inc. | +1-781-999-5354 | United States | 19973 | 58 | Inquiry |
Aladdin Scientific | +1-+1(833)-552-7181 | United States | 57511 | 58 | Inquiry |
Amadis Chemical Company Limited | 571-89925085 | China | 131980 | 58 | Inquiry |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | China | 9887 | 58 | Inquiry |
Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-400-6206333 18521732826 | China | 25013 | 65 | Inquiry |
Shanghai Aladdin Biochemical Technology Co.,Ltd. | +86-18521732826 | China | 48467 | 58 | Inquiry |
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