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 Experiment | |
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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 . |
Concentrations | ~10 μM |
Incubation time | 24 hours |
Animal Experiment | |
---|---|
Animal models | Mice bearing Colo-205 xenografts |
Formulation | |
Dosages | ~100 mg/kg |
Administration | p.o. |
Molecular Weight | 326.18 |
Formula | C14H13Cl2N3O2 |
CAS Number | 1169562-71-3 |
Solubility (25°C) | DMSO 10 mM |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
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