JNJ-38877618

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-38877618 (OMO-1) 是一种新型强效、高选择性、口服生物可利用的 c-Met 酪氨酸激酶抑制剂。

JNJ-38877618 (OMO-1) is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively; potently inhibits MET receptor phosphorylation and downstream pathway modulation in the nanomolar range and induces anti-proliferative and anti-migratory activity in models with MET gene amplification, mutant or ligand-mediated pathway activation; completely suppresses tumour growth SNU5 MET amplified gastric, U87-MG HGF autocrine glioblastoma and Hs746T MET exon 14 skipping mutant gastric cancer models.Solid Tumors Phase 1 Clinical.

OMO-1 (formerly JNJ-38877618), is a potent, highly selective, orally bioavailable Met kinase inhibitor with nM binding affinity (Kd=1.4 nM) and enzyme inhibitory activity against wt and M1268T mutant Met (2 and 3 nM IC50). Met inhibitory effects are assessed in proliferation, colony formation and motility assays. JNJ-38877618 displays nM potency against Met Ampl/mutant and therapy resistant models.

JNJ-38877618 induces complete inhibition of tumor growth in 3 models: the SNU5 Met amp gastric, U87-MG HGF autocrine glioblastoma and Hs746T Met exon 14 skipping mutant gastric cancer. JNJ-38877618 induces regression of large Met amplified EBC-1 SqNSCLC where JNJ-38877618 leads to dose- and time-dependent inhibition of Met kinase activation, with the duration of target shut down considerably exceeding plasma exposure times. Combination treatments are well tolerated and improved EGFR targeted therapy.

OMO1 | JNJ38877618 | OMO-1

Angiogenesis

c-Met/HGFR

c-Met/HGFR

Cancer

Solid Tumors

943540-74-7

374.355

C20H12F2N6

>98% (HPLC)

DMSO : 5 mg/mL 13.36 mM

FC(C1=CC=C2N=CC=CC2=C1)(F)C3=NN=C4C=CC(C5=CC=NC=C5)=NN43

6-(difluoro(6-(pyridin-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline

(-20℃)

With Ice Pack

≥ 2 years