XL413 inhibits the cell proliferation. XL413 decreases cell viability and elicits the caspase 3/7 activity in Colo-205 cells. XL413 results in modified S phase progression that subsequently leads to apoptotic cell death. XL413, at the 3 mg/kg dose, causes 70% inhibition of phosphorylated MCM2, and causes significant tumor growth regression at the 100 mg/kg dose.
|Cell lines||Colo-205 cells|
|Preparation method||Using BrdU incorporation assay to measure the cell proliferation , and by Cell Titer–Glo kits to assay viability .|
|Incubation time||24 hours|
|Animal models||Mice bearing Colo-205 xenografts|
|Solubility (25°C)||DMSO 10 mM|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Koltun ES, et al. Bioorg Med Chem Lett. Discovery of XL413, a potent and selective CDC7 inhibitor.
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