| 产品描述: | Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC). |
| 体外研究: |
Dalmelitinib (Compound 4 d, intragastric administration, 10-60 mg/kg) significantly inhibits the tumor growth in a dose-dependent manner in MKN-45 tumor xenograft nude mice. Dalmelitinib (intragastric administration, 5 mg/kg for a single dose) shows a high plasma concentration, longer half-life and mean residence time, low clearance rates in BALB/c small nude mice. Dalmelitinib shows a high level of No Observed Adverse Effect Level (NOAEL) in mice long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day). |
| 体内研究: |
Dalmelitinib (Compound 4 d) binds to the ATP-binding region of c-Met kinase, and shows slective inhibitory activity against c-Met with an IC50 value of 2.9 nM. Dalmelitinib (0-1 μM approximately, 3 days) inhibits cell proliferation in various c-Met oncogene amplification cancer cell lines, with IC50 values ranging from 6 nM to 33 nM. Dalmelitinib (0.1-1 μM, 6-24 h) significantly induces the phosphorylation of the tyrosine kinases (MET), partially or completely inhibits the downstream phosphorylation of ERK and AKT in HCCLM3 cells. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.167 ml |
10.835 ml |
21.67 ml |
| 5 mM |
0.433 ml |
2.167 ml |
4.334 ml |
| 10 mM |
0.217 ml |
1.083 ml |
2.167 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.433 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。 |