783355-60-2 Usage
Description
CRA-02478, also known as PCI-24781, is a novel hydroxamic acid histone deacetylase (HDAC) inhibitor. It is a compound that modulates the activity of histone deacetylases, which are enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. This modulation can lead to changes in gene expression and has potential therapeutic applications.
Used in Pharmaceutical Industry:
CRA-02478 is used as a histone deacetylase inhibitor for its potential role in the treatment of various diseases, including cancer. It exerts cytotoxicity and induces histone H3 alterations via caspase-8 and FADD in leukemia cells, suggesting its potential use in targeted cancer therapies.
Used in Cancer Research:
In cancer research, CRA-02478 is used as a tool to study the role of histone deacetylases in the development and progression of cancer. Its ability to modulate gene expression and induce cell death in leukemia cells highlights its potential as a therapeutic agent for the treatment of hematological malignancies and possibly other types of cancer as well.
Biological Activity
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].
Enzyme inhibitor
This broad-spectrum histone deacetylase inhibitor (FW = 394.48 g/mol; CASs = 783355-60-2, 783356-67-2 (HCl)); Solubility: 80 mg/mL DMSO; <1 mg/mL Water; Formulated in 30% HP-cyclodextrin in water), also known as CRA-024781 and systematically as 3-((dimethylamino)methyl)- N-(2-(4-(hydroxycarbamoyl)phenoxy)ethyl)benzofuran-2-carboxamide, is a novel broad-spectrum HDAC inhibitor targeting HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki of 7 nM, 19 nM, 8.2 nM, 17 nM, 280 nM, 24 nM, respectively. PCI-24781 treatment causes dosedependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells. It also induces expression of p21 and leads to PARP cleavage and accumulation of the γH2AX.
references
[1]. buggy jj, cao za, bass ke, et al. cra-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. mol cancer ther, 2006, 5(5): 1309-1317..
Check Digit Verification of cas no
The CAS Registry Mumber 783355-60-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 7,8,3,3,5 and 5 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 783355-60:
(8*7)+(7*8)+(6*3)+(5*3)+(4*5)+(3*5)+(2*6)+(1*0)=192
192 % 10 = 2
So 783355-60-2 is a valid CAS Registry Number.
InChI:InChI=1/C21H23N3O5/c1-24(2)13-17-16-5-3-4-6-18(16)29-19(17)21(26)22-11-12-28-15-9-7-14(8-10-15)20(25)23-27/h3-10,27H,11-13H2,1-2H3,(H,22,26)(H,23,25)
783355-60-2Relevant articles and documents
A method for preparing ilastatin is disclosed. Preparation method of intermediate and intermediate
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, (2021/10/27)
The preparation method comprises the following steps: (1) the first intermediate 3 - (dimethylamino) methyl) benzofuran -2 - carboxylic acid and second intermediate 4 - (2 - aminoethoxy) methyl benzoate are subjected to amide condensation to obtain third