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CVT-313 (CAS 199986-75-9)

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Synonym:2(bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine
Application:An inhibitor of Cdk2
CAS Number:199986-75-9
Purity:≥98%
Molecular Weight:400.5
Molecular Formula:C20H28N6O3
Refer to Certificate of Analysis for lot specific data (including water content).
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 Ordering Information
Product NameCatalog #UnitPriceQtyAddFavorites
CVT-313 sc-221445 1 mg $67
CVT-313 sc-221445A 5 mg $260
Description
A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 µM for Cdk2/A and Cdk2/E; 4.2 µM for Cdk1/B; 215 µM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC50 > 1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC50 ~1.25-20 µM) in vitro and prevent neointima formation in vivo.
Technical Information
Physical State:Solid
Solubility:Soluble in DMSO (10 mg/ml), DMF, and 100% ethanol.
Storage:Store at -20° C
Melting Point:268.02 °C (Predicted)
Boiling Point:652.28 °C at 760 mmHg (Predicted)
Density:1.30 g/cm3 (Predicted)
Refractive Index:n20D 1.63 (Predicted)
IC50:CDK2/cyclin A: IC50 = 500 nM; CDK2/cyclin E: IC50 = 500 nM; CDK1/cyclin B: IC50 = 4.2 µM; CDK4/cyclin D1: IC50 = 215 µM; MAPK: IC50 >1.25 mM; Induce tumor cells growth arrest: IC50 = 1.25-20 µM; Cyclin-dependent kinase 1: IC50 = 330 µM (human); PKA: IC50 >1.25 mM; PKC: IC50 >1.25 mM
pK Values:pKa: 13.95 (Predicted), pKb: 6.85 (Predicted)
Safety and Reference Information
PubChem CID:6918386
MDL Number:MFCD06411412
SMILES:CC(C)N1C=NC2=C1N=C(N=C2NCC3=CC=C(C=C3)OC)N(CCO)CCO
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation: E.E. Brooks, et al.; J. Biol. Chem. 272, 29207 (1997) 2. Histone H1 phosphorylation by Cdk2 selectively modulates mouse mammary tumor virus transcription through chromatin remodeling: R.N. Bhattacharjee, et al.; Mol. Cell. Biol. 21, 5417 (2001)
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