For research use only. Not for therapeutic Use.
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].
MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM[1].
MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM[1].
MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model[1].
MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2,CL, and F% values are 1.5 µg/mL, 10.7 µg•h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively[1].
Catalog Number | I015152 |
CAS Number | 2101241-90-9 |
Synonyms | 5-[3-fluoro-4-[7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl]oxyanilino]-3-phenyl-1H-1,6-naphthyridin-4-one |
Molecular Formula | C33H27FN4O4 |
Purity | ≥95% |
InChI | InChI=1S/C33H27FN4O4/c1-33(2,40)19-41-22-9-10-23-27(17-22)35-15-13-28(23)42-29-11-8-21(16-25(29)34)38-32-30-26(12-14-36-32)37-18-24(31(30)39)20-6-4-3-5-7-20/h3-18,40H,19H2,1-2H3,(H,36,38)(H,37,39) |
InChIKey | DGRCFAYRKDYEMX-UHFFFAOYSA-N |
SMILES | CC(C)(COC1=CC2=NC=CC(=C2C=C1)OC3=C(C=C(C=C3)NC4=NC=CC5=C4C(=O)C(=CN5)C6=CC=CC=C6)F)O |
Reference | [1]. Chen T, et al. Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate. Eur J Med Chem. 2020;192:112174. |