| 产品描述: | c-Met 抑制剂;c-Met Inhibitors;;InformationJNJ-38877618(OMO-1) JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50).TargetsMet (Cell-free assay); MET (M1268T) (Cell-free assay) 2 nM; 3 nMIn vivoOMO-1 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. Combination treatments are well tolerated and improve EGFR targeted therapy. Although single agent OMO-1 has no effect on NSCLC HCC827 EGFR, combination with Erlotinib leads to delayed onset of tumor recurrence. |
| 靶点: |
IC50: 2 nM (wt Met), 2 nM (mutant Met) |
| 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. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.671 ml |
13.356 ml |
26.713 ml |
| 5 mM |
0.534 ml |
2.671 ml |
5.343 ml |
| 10 mM |
0.267 ml |
1.336 ml |
2.671 ml |
| 50 mM |
0.053 ml |
0.267 ml |
0.534 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |