| 产品描述： | CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4. |
| 靶点： |
Others |
| 体外研究： |
In an assay using recombinant human PLK4, CFI-400945 inhibited PLK4 (IC50: 2.8 ± 1.4 nM and Ki: 0.26 ± 0.1 nM in an ATP competitive manner). CFI-400945 inhibited autophosphorylation of PLK4 at serine 305 (EC50: 12.3 nM in cells overexpressing PLK4). CFI-400945 showed no significant inhibitory activity against other PLK family members (PLK1, PLK2, and PLK3 with the IC50s of > 50 μM). In transfected HCT116 cells with TRKA, TRKB, and Tie2/TEK, the EC50 values were 84 nM, 88 nM, and 117 nM, respectively. CFI-400945 inhibited the activity of AURKA and AURKB with the EC50 value of 510 nM and 102 nM. CFI-400945 (≥ 200 nM) decreased the mean centriole number in asynchronous U2OS cells. CFI-400945 inhibited a panel of breast cancer cell growth with the GI50 of 14-165 nM |
| 体内研究： |
In mice, the maximum tolerated dose (MTD) of CFI-400945 for once-daily oral administration was estimated to be 7.5-9.5 mg/kg |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 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 |
1.537 ml |
7.684 ml |
15.368 ml |
| 5 mM |
0.307 ml |
1.537 ml |
3.074 ml |
| 10 mM |
0.154 ml |
0.768 ml |
1.537 ml |
| 50 mM |
0.031 ml |
0.154 ml |
0.307 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京