XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 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.

CDC7:3.4 nM, Pim1:42 nM, CK2:212 nM

XL413 (BMS-863233) hydrochloride effectively inhibits cell proliferation (IC 50 = 2685 nM), reduces cell viability (IC 50 = 2142 nM), and increases caspase 3/7 activity (EC 50 = 2288 nM) in Colo-205 cells. Additionally, it significantly suppresses the anchorage-independent growth of Colo-205 cells in soft agar (IC 50 = 715 nM) [1]. Demonstrating cytotoxic effects, XL413 hydrochloride has IC 50 values of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. It triggers apoptosis in Colo-205 cells without affecting HCC1954 cells. As a DDK inhibitor, XL413 shows potent activity in vitro (IC 50 = 22.7 nM), yet fails to inhibit DDK-dependent Mcm2 phosphorylation in HCC1954 cells, while remaining effective in Colo-205 cells [2].

XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposure and favorable pharmacokinetic properties in mice. Additionally, XL413 hydrochloride (10, 30, or 100 mg/kg, p.o.) is well tolerated at all tested doses without significant body weight loss [1].