产品说明书
SYN1143
 |
同义名 : | AMG-1;c-Met/RON Dual Kinase Inhibitor;Met Kinase Inhbitor IV;Ron Inhibitor I;RON inhibitor 1;RON-IN-1 |
| CAS号 : | 913376-84-8 | |
| 货号 : | A1212551 | |
| 分子式 : | C31H29FN4O5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 556.584 | |
| MDL号 : | MFCD22631502 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(188.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Recepteur d'origine nantais (RON) and c-Met are receptor tyrosine kinases involved in cell proliferation, migration, and invasion, all of which are key biological events in tumorigenesis. RON-IN-1 is a potent inhibitor of both RON and c-Met that selectively inhibited their kinase activities with IC50 values of 9nM and 4nM, respectively. It shows weak inhibitory activity towards Lck, Tie2, Src, and BTK with IC50 values ranging from 160 to 710nM. In HT-29 and BxPC3 cells, RON-IN-1 at 10 – 1000nM inhibited hepatocyte growth factor-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner. RON-IN-1 at 10 – 1000nM also inhibited NIH3T3 TPR-Met cell migration. In NIH3T3 RON and BxPC3 cells, treatment with RON-IN-1 (10 – 1000nM) dose-dependently inhibited RON signaling and functional activity. Treatment of NIH3T3 TPR-Met tumor-bearing mice with RON-IN-1 (30 or 100mg/kg once daily, or 30mg/kg twice daily) significantly inhibited tumor growth compared with vehicle-treated control animals. RON-IN-1 (30 or 100mg/kg once daily) also significantly and dose-dependently reduced tumor growth in mice bearing established HT-29 tumors[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.80mL 0.36mL 0.18mL |
8.98mL 1.80mL 0.90mL |
17.97mL 3.59mL 1.80mL |
| 参考文献 |
|---|