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產品描述： 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. |
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靶點：
Cdc7:3.4 nM (IC50);PIM1:42 nM (IC50);CK2:215 nM (IC50) |
體內研究：
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 |
參考文獻：
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. |
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溶解性：
H2O : 10 mg/mL (30.66 mM; Need ultrasonic) DMSO : 3.4 mg/mL (10.42 mM; Need ultrasonic and warming) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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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 |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京