943540-74-7

JNJ-38877618 (OMO-1) is a potent, highly selective, and orally bioavailable Met (c-Met) kinase inhibitor with a Kd of 1.4 nM. Its IC50 values for wild-type Met (c-Met) and mutant Met (c-Met) (M1268T) were 2 nM and 3 nM, respectively.

In vivo, JNJ-38877618(OMO-1) completely inhibited tumor growth in 3 tumor models: SNU5 MET amp gastric cancer model, U87-MG HGF autocrine glioblastoma model, and exon 14 skipping deletion mutation Hs746T gastric cancer model of MET gene. Administration of OMO-1 in combination with other drugs is well tolerated and can improve and enhance the effect of EGFR-targeted therapy. Although single-agent OMO-1 has no effect on NSCLC HCC827 EGFR, its combination with erlotinib can delay tumor recurrence.

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Target	Value
Met (Cell-free assay)	2 nM
MET (M1268T) (Cell-free assay)	3 nM