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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 | |
|---|---|
| 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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