CVT-313 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.

CVT-313  (CAS 199986-75-9)

CVT-313 is rated 5.0 out of 5 by 1.
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| See 4 Citations
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 NAME CATALOG # UNIT PRICE QTY FAVORITES
CVT-313 sc-221445 1 mg $69.00
CVT-313 sc-221445A 5 mg $268.00

CVT-313 is 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). It inhibits other kinases only at much higher concentrations.


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)

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)
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)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
6918386
MDL Number :
MFCD06411412
SMILES :
CC(C)N1C=NC2=C1N=C(N=C2NCC3=CC=C(C=C3)OC)N(CCO)CCO

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Certificate of Analysis

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CVT-313 Product Citations

See how others have used CVT-313. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 27109354
Chen, X. et al. 2016. Nuclear phosphoproteomics analysis reveals that CDK1/2 are involved in EGF-regulated constitutive pre-mRNA splicing in MDA-MB-468 cells. Journal of proteomics.

PMID: # 25149358
Zalzali, H. et al. 2015. CDK2 transcriptional repression is an essential effector in p53-dependent cellular senescence-implications for therapeutic intervention. Molecular cancer research : MCR. 13: 29-40.

PMID: # 26606677
Paiva, C. et al. 2015. Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. PloS one. 10: e0143685.

PMID: # 22548705
Zalzali, H. et al. 2012. Temporally distinct roles for tumor suppressor pathways in cell cycle arrest and cellular senescence in Cyclin D1-driven tumor. Molecular cancer. 11: 28.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Brooks Brooks, EE. et al. (PubMed 9360999) reported that CVT-313, a specific and potent inhibitor of CDK2, prevents neointimal proliferation. -SCBT Publication Review
Date published: 2015-07-13
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