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XL413

Cat. No. M3641
XL413 Structure
Synonym:

BMS-863233

Size Price Availability Quantity
5mg USD 132  USD132 In stock
10mg USD 185  USD185 In stock
50mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Koltun ES, et al. Bioorg Med Chem Lett. Discovery of XL413, a potent and selective CDC7 inhibitor.

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