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XL413 is a potent inhibitor of Cdc7 (IC50 = 3.4 nM).1 It is >60, >10, and >300-fold selective for Cdc7 over CK2, PIM1, and a panel of over 100 protein kinases, respectively. XL413 inhibits the growth of MDA-MB-231T and COLO 205 cells (IC50s = 118 and 140 nM, respectively). It inhibits Cdc7-specific phosphorylation of mini-chromosome maintenance protein (MCM2) and induces cell cycle accumulation in the S and G2 phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7. In vivo, XL413 inhibits MCM2 phosphorylation (ED50 = <3 mg/kg) and reduces tumor growth in a COLO 205 mouse xenograft model when administered orally at doses of 10, 30, and 100 mg/kg.
WARNING This product is not for human or veterinary use.
1. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg. Med. Chem. Lett. 22(11), 3727-3731 (2012).