| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
cdk2/cyclin A (IC50 = 0.5 μM); Cdk1/cyclin B (IC50 = 4.2 μM); Cdk4/cyclin D1 (IC50 = 215 μM)
CVT-313 targets cyclin-dependent kinase 2 (CDK2). It acts as a potent, selective, reversible, and ATP-competitive inhibitor. It has an IC50 of 0.5 μM for CDK2/A and CDK2/E. It also inhibits CDK5 in the sub-micromolar range (IC50 = 0.42 μM). |
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| ln Vitro |
CVT-313 causes cells to become less prone to hyperphosphorylation of the retinoblastoma gene product, which stops cell cycle progression at the G1/S junction. With an IC50 for growth arrest ranging from 1.25 to 20 μM, CVT-313 also inhibits the growth of human, rat, and mouse cells in culture. CVT-313 inhibits Rb hyperphosphorylation[1].
CVT-313 inhibits CDK2 with an IC50 of 0.5 μM. It inhibits CDK5 with an IC50 of 0.42 μM. It has IC50 values of 4.2 μM for CDK1/B and 215 μM for CDK4/D1. Inhibition is competitive with respect to ATP (Ki=95 nM) and selective. |
| ln Vivo |
In vivo activity data for CVT-313 is limited. As a CDK2 inhibitor, it is expected to have effects on cell cycle progression and tumor growth. The compound is used as a research tool to study the role of CDK2 in cell cycle regulation.
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| Enzyme Assay |
Purified CDC5L(295-795)-His6 is combined with [γ-32P]ATP and COS-7 cell extract for kinase assays. The mixture is then incubated in 30°C for 10 minutes at 100 μL of 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM NaVO3, and the specific inhibitor. Subconfluent, serum-stimulated COS-7 cells are lysed in 20 mM HEPES-NaOH, pH 7.5, 50 mM NaCl, 1% Triton X-100, 10% glycerol, protease, and phosphotase inhibitors to prepare cell extract, which is used as a source of kinase activity. In 15% polyacrylamide-SDS gels, phosphorylated proteins are separated by electrophoresis. 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS, and 50 μM PD98059 were among the particular inhibitors[1].
CVT-313 is evaluated in cell-free kinase assays using purified CDK2 and other cyclin-dependent kinases. The compound is incubated with the kinase, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of CDK inhibition. |
| Cell Assay |
The culture medium for MRC-5 cells is Dulbecco's modified Eagle's medium supplemented with 5% fetal calf serum. Cells growing exponentially in tissue culture are supplemented with CVT313 (0, 5, 10, 15 μM). One measures the cell population. After 48 hours of exposure, proliferation assays are performed with the nonradioactive CellTiter 96 kit. Trypsinized cells are fixed in 70% ice-cold ethanol, treated with 40 μg/mL propidium iodide and 0.1 mg/mL RNase A for 1 hour at 37°C, and then their DNA content is analyzed using FACS[2].
CVT-313 is assessed in cell-based assays using various cancer cell lines. Cells are treated with CVT-313, and cell cycle progression, cell proliferation, and apoptosis are measured. CDK2 activity and phosphorylation of downstream targets are assessed by Western blot analysis. |
| Animal Protocol |
CVT-313 is administered in animal models to evaluate its effects on tumor growth. However, specific animal study protocols are not extensively documented. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
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| ADME/Pharmacokinetics |
CVT-313 has a molecular weight of 349.39 and a molecular formula of C18H23N7O. It has a CAS number of 199986-75-9. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CVT-313. The compound is for research use only and is not intended for human therapeutic use. It is a potent CDK2 inhibitor.
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| References | |
| Additional Infomation |
CVT-313 is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2. It is also known as NG-26 and Cdk2 Inhibitor III. It is used in research on cell cycle regulation and cancer. It is not approved for clinical use.
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| Molecular Formula |
C20H28N6O3
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|---|---|
| Molecular Weight |
400.483
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| Exact Mass |
400.222
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| Elemental Analysis |
C, 59.98; H, 7.05; N, 20.99; O, 11.98
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| CAS # |
199986-75-9
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| Related CAS # |
199986-75-9
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| PubChem CID |
6918386
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| Appearance |
White to off-white solid powder
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| Density |
1.3g/cm3
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| Boiling Point |
652.3ºC at 760 mmHg
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| Flash Point |
348.3ºC
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| Vapour Pressure |
6.65E-18mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
1.891
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])O[H])C1=NC(=C2C(=N1)N(C([H])=N2)C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H]
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| InChi Key |
NQVIIUBWMBHLOZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H28N6O3/c1-14(2)26-13-22-17-18(21-12-15-4-6-16(29-3)7-5-15)23-20(24-19(17)26)25(8-10-27)9-11-28/h4-7,13-14,27-28H,8-12H2,1-3H3,(H,21,23,24)
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| Chemical Name |
2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol
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| Synonyms |
CVT313 CVT 313 CVT-313
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (~249.7 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4970 mL | 12.4850 mL | 24.9700 mL | |
| 5 mM | 0.4994 mL | 2.4970 mL | 4.9940 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4970 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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