XL413 (BMS-863233) hydrochloride 是一种有效的,选择性的,ATP 竞争性的Cdc7抑制剂,IC50值为 3.4 nM。XL413 (BMS-863233) hydrochloride对 CK2 和 Pim1 的IC50值分别为 215 和 42 nM,对 pMCM 的EC50值为 118 nM。
产品描述
XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 (BMS-863233) hydrochloride also exhibits potent effect with IC 50 s of 215, 42 nM on CK2, PIM1, respectively, and an EC 50 of 118 nM on pMCM.
体外活性
XL413 (BMS-863233) hydrochloride inhibits the cell proliferation (IC 50 =2685 nM), decreases cell viability (IC 50 =2142 nM) and elicits the caspase 3/7 activity (EC 50 =2288 nM) in Colo-205 cells. XL413 hydrochloride also markedly inhibits the anchorage-independent growth of colo-205 in soft agar (IC 50 =715 nM) [1]. XL413 hydrochloride exhibits cytotoxic effects on tumors, with IC 50 of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. XL413 hydrochloride induces apoptosis in the Colo-205 cells, while not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC 50 of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells [2].
体内活性
XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride exhibits 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 without significant body weight loss [1].
Cas No.
2062200-97-7
分子式
C14H13Cl2N3O2
分子量
326.18
别名
XL413;BMS-863233 Hydrochloride;BMS-863233
储存和溶解度
DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years