S81223 |
XL413 |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)