JNJ-38877618是一种有效的，高选择性的，口服可用的 (Met) 激酶抑制剂，对于野生型和突变体的 IC₅₀ 值分别为2和3 nM。

JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC 50 s of 2 and 3 nM for wild type and mutant Met, respectively.

Solid

IC50: 2 nM (wt Met), 2 nM (mutant Met)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Libouban M, et al. OMO-1, a potent, highly selective, orally bioavailable, Met kinase inhibitor with a favorable preclinical toxicity profile, shows both monotherapy activity, against Met pathway-driven tumors, and EGFR TKI combination activity in acquire

In Vitro: DMSO : 5 mg/mL (13.36 mM; Need ultrasonic)配制储备液