1D-2

1D-2 is a c-Met protein kinase inhibitor, with a human-derived IC₅₀ of 1.45 nM. 1D-2 inhibits the proliferation of cancer cells and exhibits metabolic stability in human and rat liver microsomes. 1D-2 can be used in related research on non-small cell lung cancer^[1]. In Vitro:1D-2 (72 h) potently inhibits the proliferation of human non-small cell lung cancer NCI-H1993 cells, with an IC₅₀ value of 24.7 nM^[1].
1D-2 (5-10 min preincubation, 30 min kinase reaction, 1 h detection incubation) potently inhibits the activity of purified c-Met kinase, with an IC₅₀ of 1.45 nM^[1].
1D-2 (1 μM; preincubated for 5 min, followed by incubation with NADPH for 5-30 min) exhibits favorable metabolic stability in human liver microsomes (CL_int = 8 μl/min/mg protein) and rat liver microsomes (CL_int = 49 μl/min/mg protein)^[1].
1D-2 (10 μM; preincubated for 5 min, followed by incubation with NADPH for 5-30 min) directly inhibits CYP2C9 in human liver microsomes, and exhibits no time-dependent inhibitory effect on all tested cytochrome P450 isoforms^[1].
1D-2 exhibits extremely high selectivity for c-Met, with IC₅₀ values > 1000 nM against the other 17 tested human tyrosine kinases ^[1].