| Cas No.: | 1173699-31-4 |
| Chemical Name: | Amg-337 |
| Synonyms: | AMG-337;Compound M;(R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one;AMG337;AMG 337;08WG8S0L8D;1,6-Naphthyridin-5(6H)-one, 6-[(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-;1,6-Naphthyridin-5(6H)-one, 6-((1R)-1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo(4,3-a)pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-;AMG 337 [WHO-DD];BCP16602;s8167;BDBM50157612;SB19194;A16400 |
| SMILES: | FC1=C([H])C(C2C([H])=NN(C([H])([H])[H])C=2[H])=C([H])N2C1=NN=C2[C@@]([H])(C([H])([H])[H])N1C([H])=C([H])C2=C(C([H])=C(C([H])=N2)OC([H])([H])C([H])([H])OC([H])([H])[H])C1=O |
| Formula: | C23H22FN7O3 |
| M.Wt: | 463.4643 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays. |
| In Vivo: | AMG-337 demonstrates robust activity in MET-dependent cancer models. Oral administration of AMG 337 results in robust dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, with inhibition of tumor growth consistent with the pharmacodynamic modulation of MET signaling.[1] |
| In Vitro: | AMG-337 demonstrates exquisite selectivity for MET when profiled against a diverse panel of over 400 protein and lipid kinases in a competitive binding assay. In cellular assays, AMG 337 inhibits HGF-dependent MET phosphorylation with an IC50 of < 10 nM. [1] AMG 337 is a selective inhibitor of Met, which inhibits multiple mechanisms of Met activation. [2] |
| References: | [1]. Paul E. Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728 [2]. Cecchi F, et al. Targeting the HGF/Met signaling pathway in cancer therapy. Expert Opin Ther Targets. 2012 Jun;16(6):553-572. |
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COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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