Name: PCI-24781 (CRA-024781)
Price: 255.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CRA-024781 is a novel HDAC inhibitor targeting HDAC1, HDAC2, HADC3, HADC6, HADC8, HADC10 with IC50 value of 7 nM(Ki), 19 nM(Ki), 8.2 nM(Ki), 17 nM(Ki), 280 nM(Ki), 24 nM(Ki), respectively [1]. Histone deacetylases (HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. CRA-024781 exhibits potent antitumor activity against ten human tumor cell lines with GI50 ranging from 0.15 μM to 3.09 μM. CRA-024781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 μM. CRA-024781 treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells suggesting that HDAC enzymes are inhibited in these cells. CRA-024781 also induces the expression of p21 (a protein playing a role in the antitumor effect) and leads to PARP cleavage and accumulation of the γH2AX, which indicate apoptosis [1]. Treatment with CRA-024781 at 200 mg/kg once daily every other day significantly inhibits the growth of HCT116 and DLD-1 xenografts in mice by 69% and 59%, respectively. In the HCT116 model, treatment with CRA-024781 at 20 mg/kg, 40 mg/kg, 80 mg/kg, or 160 mg/kg (q.d. × 4 per week) causes inhibition of tumor growth by 48%, 57%, 82.2%, or 80.0%, respectively [1].
- Properties
  - Alternative Name
    
    3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide
    
    CAS Number
    
    783355-60-2
    
    Molecular Formula
    
    C21H23N3O5
    
    Molecular Weight
    
    397.42
    
    Appearance
    
    A solid
    
    Purity
    
    98.01%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥11.75 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

PCI-24781 (CRA-024781)

PCI-24781 (CRA-024781)

Background

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