XL413 (hydrochloride) 化学特性,用途語,生産方法
説明
XL413 is a potent inhibitor of Cdc7 (IC
50 = 3.4 nM). 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 (IC
50s = 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 G
2 phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7.
In vivo, XL413 inhibits MCM2 phosphorylation (ED
50 = <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.
XL413 (hydrochloride) 上流と下流の製品情報
原材料
準備製品