化合物JNJ-38877618 T15617

Product Introduction
Bioactivity


英文名: JNJ-38877618

描述: JNJ-38877618 (OMO-1)是一种口服有活性的 Met 激酶选择性抑制剂，其对野生型和突变体的 IC50值分别为2和3 nM。

体外活性: JNJ-38877618 shows nM potency against Met Ampl/mutant and therapy-resistant models. JNJ-38877618 has 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.

体内活性: JNJ-38877618 results in the 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. JNJ-38877618 causes 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. Combination treatments are well tolerated and improved EGFR targeted therapy[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.5 mg/mL (12.02 mM)


关键字: JNJ 38877618 | OMO 1 | Inhibitor | c-Met/HGFR | JNJ38877618 | JNJ-38877618 | inhibit | OMO1

相关产品: Savolitinib | SU11274 | c-Met-IN-2 | Cabozantinib | c-Met-IN-18 | BMS-794833 | Hepln-13 | BMS817378 | Golvatinib | NVP-TAE 226

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Highly Selective Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途