产品
编 号:F253683
分子式:C14H13Cl2N3O2
分子量:326.18
产品类型
结构图
CAS No: 2062200-97-7
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产品详情
生物活性:
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.
体外研究:
XL413 (BMS-863233) hydrochloride inhibits the cell proliferation (IC50=2685 nM), decreases cell viability (IC50=2142 nM) and elicits the caspase 3/7 activity (EC50=2288 nM) in Colo-205 cells. XL413 hydrochloride also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC50=715 nM). XL413 hydrochloride shows cytotoxic effects on tumors, with IC50 of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. XL413 hydrochloride induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC50 of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells.