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.
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.
溶解度： H2O : 10 mg/mL (30.66 mM; Need ultrasonic) DMSO : 3.4 mg/mL (10.42 mM; Need ultrasonic and warming)
