AMG 458
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AMG 458 속성
- 밀도
- 1.339
- 저장 조건
- Store at -20°C
- 용해도
- DMSO에 용해됨
- 물리적 상태
- 가루
- 색상
- Off-white to pink
안전
AMG 458 C화학적 특성, 용도, 생산
효소 저해제
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 준비 용품 및 원자재
원자재
준비 용품
AMG 458 공급 업체
글로벌( 70)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 25604 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 |
sales@sarms4muscle.com | China | 10522 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 |
sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 |
support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 |
sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 |
sales@amadischem.com | China | 131980 | 58 |
| Chembest Research Laboratories Limited | 021-20908456 |
sales@BioChemBest.com | China | 6008 | 61 |
| Jinan Trio PharmaTech Co., Ltd. | +86 (531) 88811783 |
sales@trio-pharmatech.com (International market) | China | 1856 | 62 |