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CVT-313

Cat. No. M8902
CVT-313 Structure
Synonym:

NG26

Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CVT-313 is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 wirh IC50 of 0.5 μM. Inhibition is competitive with respect to ATP (Ki=95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity.

Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC50 for growth inhibition ranged from 1.25 to 20 μM. CVT-313 is a promising candidate for evaluation in other disease models related to aberrant cell proliferation.

Protocol
Cell Experiment
Cell lines MRC-5 cells
Preparation method CVT-313 is prepared in DMSO and stored, and then diluted with appropriate medium before use.
MRC-5 cells are grown in Dulbecco’s modified Eagle’s medium containing 5% fetal calf serum. CVT-313 (0, 5, 10, 15 μM) is added to exponentially growing cells in tissue culture. Cell population is measured. Proliferation assays are carried out using the nonradioactive CellTiter 96 kit after 48-h exposure. For FACS analysis of DNA content, cells are trypsinized, fixed in 70% ice-cold ethanol, and treated with 0.1 mg/mL RNase A and 40 μg/mL propidium iodide for 1 h at 37°C.
Concentrations 0, 5, 10, 15 μM
Incubation time 48 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 400.47
Formula C20H28N6O3
CAS Number 199986-75-9
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing.
Graub R, et al. Cell Cycle. 2008 Jun 15;7(12):1795-803. PMID: 18583928.

CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation.
Brooks EE, et al. J Biol Chem. 1997 Nov 14;272(46):29207-11. PMID: 9360999.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CVT-313, NG26 supplier, CDK, inhibitors

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