XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor ofCdc7, with anIC₅₀of 3.4 nM, and also shows potent effect withIC₅₀s of 215, 42 nM onCK2,PIM1, respectively, and anEC₅₀of 118 nM on pMCM.

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)^[1].
XL413 hydrochloride shows cytotoxic effects on tumors, with IC₅₀of 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 IC₅₀of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells^[2].

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^[1].

326.18

Solid

C₁₄H₁₃Cl₂N₃O₂

2062200-97-7

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : 10 mg/mL(30.66 mM;Need ultrasonic)

DMSO : 3.4 mg/mL(10.42 mM;Need ultrasonic and warming)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。