XL413 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 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 also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC₅₀= 715 nM)^[1]. XL413 shows cytotoxic effects on tumors, with IC₅₀of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. XL413 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 is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells^[2].

XL413 (100 mg/kg, p.o.) shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) is well tolerated at all the doses, with no significant body weight loss^[1].

289.72

C₁₄H₁₂ClN₃O₂

1169558-38-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.