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|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Discovery of XL413, a potent and selective CDC7 inhibitor.
Koltun ES, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. PMID: 22560567.
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Voruciclib (P1446A-05) is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with IC50s of 90nM, 25nM, and 22nM for CDK4-CyclinD1, CDK1-Cyclin B, and CDK9-Cyclin T, respectively.
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