JNJ-38877618

JNJ-38877618CAS号: 943540-74-7分子式: C20H12F2N6分子量: 374.35描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO : 5 mg/mL (13.36 mM; Need ultrasonic)
生物活性
In vitro(体外研究)
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.
In vivo(体内研究)
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.