AMG-337
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C23H22FN7O3
- MW: 463.46
Description
AMG-337 is an orally bioavailable, potent and exquisitely selective inhibitor of wild-type and some mutant forms of c-Met. In competitive binding assays on 402 human kinases, enantiomerically (optically) pure AMG-337 hits c-Met only (with an IC50 < 5 nM). In a cell viability study, the only cell lines that responded to an AMG 337 were gastric cancer cells harboring c-Met gene amplification. None of the other cell lines were sensitive to the AMG-337 and none harbored c-Met gene amplification. It inhibited HGF-dependent c-Met phosphorylation with an IC50 of less than 10 nM in cellular assay. Orally administered AMG-337 in c-Met amplified gastric cancer xenograft models resulted in a robust dose-dependent anti-tumor efficacy.
More Information
| Parent CAS No. | 1173699-31-4 |
|---|---|
| Chemical Name | (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 |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(C2=CN(C)N=C2)=CN2C([C@@H](C)N3C(=O)C4C=C(OCCOC)C=NC=4C=C3)=NN=C2C(F)=C1 |&1:10,r| |
| MFCD | N.A. |
| 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 |
| CID | 44181686 |
| Short Description | c-Met kinase inhibitor |
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