XL413 hydrochloride

XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7 , with an IC 50 of 3.4 nM, and also shows potent effect with IC 50 s of 215, 42 nM on CK2 , PIM1 , respectively, and an EC 50 of 118 nM on pMCM. In Vitro XL413 (BMS-863233) hydrochloride inhibits the cell proliferation (IC 50 =2685 nM), decreases cell viability (IC 50 =2142 nM) and elicits the caspase 3/7 activity (EC 50 =2288 nM) in Colo-205 cells. XL413 hydrochloride also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC 50 =715 nM). XL413 hydrochloride shows cytotoxic effects on tumors, with IC 50 of 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 IC 50 of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC 50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:Cdc7 3.4 nM (IC 50 ) PIM1 42 nM (IC 50 ) CK2 215 nM (IC 50 )

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