For research use only. Not for therapeutic Use.
AMG-337（Cat No.:I000616）is a highly selective small-molecule inhibitor of the MET receptor tyrosine kinase, which plays a crucial role in cell growth, survival, and metastasis in various cancers. By specifically targeting the MET signaling pathway, AMG-337 blocks the activation of downstream pathways involved in tumor development, particularly in cancers with MET amplification or overexpression. It has shown promising results in preclinical and early clinical trials, particularly for gastric and esophageal cancers. AMG-337 is being studied for its potential to treat MET-driven malignancies and improve cancer therapy outcomes.
| Catalog Number | I000616 |
| CAS Number | 1173699-31-4 |
| Synonyms | (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 |
| Molecular Formula | C23H22FN7O3 |
| Purity | ≥95% |
| Target | c-MET |
| Solubility | DMSO: ≥ 30 mg/mL |
| Storage | Store at -20°C |
| IC50 | 5nM |
| IUPAC Name | 6-[(1R)-1-[8-fluoro-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-1,6-naphthyridin-5-one |
| InChI | InChI=1S/C23H22FN7O3/c1-14(30-5-4-20-18(23(30)32)9-17(11-25-20)34-7-6-33-3)21-27-28-22-19(24)8-15(13-31(21)22)16-10-26-29(2)12-16/h4-5,8-14H,6-7H2,1-3H3/t14-/m1/s1 |
| InChIKey | DWHXUGDWKAIASB-CQSZACIVSA-N |
| SMILES | C[C@H](C1=NN=C2N1C=C(C=C2F)C3=CN(N=C3)C)N4C=CC5=C(C4=O)C=C(C=N5)OCCOC |
| Reference | </br>1:In Vitro and In Vivo Activity of AMG 337, a Potent and Selective MET Kinase Inhibitor, in MET-Dependent Cancer Models. Hughes PE, Rex K, Caenepeel S, Yang Y, Zhang Y, Broome MA, Kha HT, Burgess TL, Amore B, Kaplan-Lefko PJ, Moriguchi J, Werner J, Damore MA, Baker D, Choquette DM, Harmange JC, Radinsky R, Kendall R, Dussault I, Coxon A.Mol Cancer Ther. 2016 Jul;15(7):1568-79. doi: 10.1158/1535-7163.MCT-15-0871. Epub 2016 Apr 19. PMID: 27196782 </br>2:Preclinical Evaluation of AMG 337, a Highly Selective Small Molecule MET Inhibitor, in Hepatocellular Carcinoma. Du Z, Caenepeel S, Shen Y, Rex K, Zhang Y, He Y, Tang ET, Wang O, Zhong W, Zhou H, Huang J, Huang E, Hu L, Coxon A, Zhang M.Mol Cancer Ther. 2016 Jun;15(6):1227-37. doi: 10.1158/1535-7163.MCT-15-0745. Epub 2016 Mar 29. PMID: 27196749 </br>3:Discovery of (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 (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC.J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11. PMID: 26812066 |
