| 产品描述： | (1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity |
| 靶点： |
PLK3:0.6 nM (IC50) |
| 体内研究： |
(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth[1].The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng•h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%. Animal Model: 6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model) Dosage: 25 mg/kg Administration: Intraperitoneal injection; daily for 21 days Result: Effective in a mouse xenograft model of tumor growth. In this study, (1E)-CFI-400437 is weighed and suspended in PEG400:water (30:70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at −20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose. |
| 参考文献： |
1. Laufer R, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087. |
| 溶解性： |
Soluble in DMSO、H2O |
| 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 |
1.768 ml |
8.842 ml |
17.684 ml |
| 5 mM |
0.354 ml |
1.768 ml |
3.537 ml |
| 10 mM |
0.177 ml |
0.884 ml |
1.768 ml |
| 50 mM |
0.035 ml |
0.177 ml |
0.354 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