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AMG-337

AMG-337

  • CAT Number: I000616
  • CAS Number: 1173699-31-4
  • Molecular Formula: C23H22FN7O3
  • Molecular Weight: 463.5
  • Purity: ≥95%
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AMG-337 (Cat.No:I000616) is an investigational, orally bioavailable, small-molecule inhibitor of the FGF receptor (FGFR) tyrosine kinase. It selectively inhibits the FGFR1, FGFR2, and FGFR3 isoforms and has shown antitumor activity in preclinical studies. AMG-337 is being developed as a potential therapy for patients with FGFR-driven solid tumors. Clinical trials are ongoing to assess its safety and efficacy.

Catalog Number I000616
CAS Number 1173699-31-4
Molecular Formula

C23H22FN7O3

Purity 95%
Target c-MET
Solubility DMSO: ≥ 30 mg/mL
Storage Store at -20°C
IC50 < 5nM [1]
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 COCCOC1=CN=C(C=CN([C@H](C)C2=NN=C3N2C=C(C4=CN(C)N=C4)C=C3F)C5=O)C5=C1
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

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