Table 1.

Profiling of NVP-BVU972 in biochemical and cellular assays

AssayIC50 ± SD, nmol/Ln
MET kinase assay14 ± 1.74
62 Other kinase assays>1,000/>10,0004
Proliferation (GTL-16)66 ± 133
Proliferation (EBC-1)32 ± 163
Proliferation (MKN-45)82 ± 62
MET phosphorylation (GTL-16)7.3 ± 2.24
MET phosphorylation (A549)221
Proliferation (BaF3 TPR-MET)104 ± 423
Proliferation (13 other BaF3 strains)>10,0001

NOTE: Biochemical activity of NVP-BVU972 was measured against MET and a panel of 62 other kinases. Inhibition of proliferation was determined in MET-amplified GTL-16, EBC-1, and MKN-45 human cancer cells as well as in transformed mouse BaF3 cells containing a panel of oncogenic kinase fusions including TPR-MET as well as parental interleukin-3-dependent BaF3 cells. Inhibition of MET autophosphorylation and HGF-stimulated MET phosphorylation was measured in GTL-16 and A549 cells, respectively. All IC50 values are given in nmol/L with SD and number of independent replicates (n).