| 产品描述： | XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM. |
| 靶点： |
Cdc7:3.4 nM (IC50);PIM1:42 nM (IC50);CK2:215 nM (IC50) |
| 体内研究： |
XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) hydrochloride is well tolerated at all the doses, with no significant body weight loss |
| 参考文献： |
1. Koltun ES, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. 2. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. |
| 溶解性： |
H2O : 10 mg/mL (30.66 mM; Need ultrasonic) DMSO : 3.4 mg/mL (10.42 mM; Need ultrasonic and warming) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.066 ml |
15.329 ml |
30.658 ml |
| 5 mM |
0.613 ml |
3.066 ml |
6.132 ml |
| 10 mM |
0.307 ml |
1.533 ml |
3.066 ml |
| 50 mM |
0.061 ml |
0.307 ml |
0.613 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