CVT-313

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CVT-313 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) with IC50 value of 0.5 μM [1].CDK2 is a serine/threonine kinase that is essential for the G1-S phase during cell division. CDK2 is an important target for prevention of aberrant cell proliferation [1].In MRC-5 cells, CVT-313 inhibited Rb hyperphosphorylation in a time-dependant way and the cell cycle was arrested at the G1/S phase. Also, CVT-313 inhibited the growth of mouse, rat and human cells with IC50 values from 1.25 to 20 mM [1]. In human diffuse large B-cell lymphoma (DLBCL) cells, CVT-313 reduced CDK2-mediated phosphorylation of the retinoblastoma gene product (Rb) on T821. Also, CVT-313 reduced the anti-apoptotic factor Myeloid cell leukemia-1 (Mcl-1) and induced apoptosis [2]. In the injured rat carotid artery model of restenosis, CVT-313 (1.25 mg/kg) reduced neointima formation by 80%. Moreover, Treatment animals with CVT-313, the neointimal areas were inhibited by at least 70%. These suggested that CDK2 was an antiproliferative target and CVT-313 is an ideal candidate for the treatment of proliferative diseases [1].
    
    [1]. Brooks EE, Gray NS, Joly A, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem, 1997, 272(46): 29207-29211.
    [2]. Faber AC, Chiles TC. Inhibition of cyclin-dependent kinase-2 induces apoptosis in human diffuse large B-cell lymphomas. Cell Cycle, 2007, 6(23): 2982-2989.
- Properties
  - Alternative Name
    
    CVT 313;NG 26;CVT313;NG26;NG-26; 2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol
    
    CAS Number
    
    199986-75-9
    
    Molecular Formula
    
    C20H28N6O3
    
    Molecular Weight
    
    400.47
    
    Appearance
    
    A solid
    
    Purity
    
    98.04%
    
    Solubility
    
    ≥20 mg/mL in DMSO; insoluble in H2O; ≥51.1 mg/mL in EtOH with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Yuan J, Jiang YY, et al. "Super-Enhancers Promote Transcriptional Dysregulation in Nasopharyngeal Carcinoma." Cancer Res. 2017 Dec 1;77(23):6614-6626. PMID:28951465

CVT-313

Background

We Also Recommend

CX-6258

CYT387 sulfate salt

CZC24832