| Identification | Back Directory | [Name]
CRA-02478 | [CAS]
783355-60-2 | [Synonyms]
CS-423
CRA 24781
CRA-02478
PCI-24781
CRA 024781
Abexinostat
PCI-24781, >=98%
PCI-24781;CRA-02478
CRA-02478 PCI-24781
PCI-24781(CRA-024781)
Abexinostat(PCI-24781)
PCI-24781 (Abexinostat)
CRA 024781;CRA 24781;ABEXINOSTAT
PCI-24781 (ABEXINOSTAT);PCI 24781
CRA 024781;CRA 24781;PCI 24781;ABEXINOSTAT
CRA-024781; CRA 024781; CRA024781; PCI24781; PCI-24781; PCI 24781; ABEXINOSTAT.
3-((diMethylaMino)Methyl)-N-(2-(4-(hydroxycarbaMoyl)phenoxy)ethyl)benzofuran-2-carboxaMide
3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide
3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide
2-Benzofurancarboxamide, 3-[(dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-
3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide PCI-24781 | [EINECS(EC#)]
811-183-9 | [Molecular Formula]
C21H23N3O5 | [MDL Number]
MFCD10565969 | [MOL File]
783355-60-2.mol | [Molecular Weight]
397.42 |
| Chemical Properties | Back Directory | [Melting point ]
198-202oC (dec.) | [density ]
1.284 | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly, Heated) | [form ]
Solid | [color ]
White |
| Hazard Information | Back Directory | [Uses]
PCI-24781 is a novel hydroxamic acid HDAC inhibitor (histone deacetylase inhibitor). ?PCI-24781 exerts cytotoxicity and histone H3 alterations via caspase-8 and FADD in leukemia cells. | [Definition]
ChEBI: 3-[(dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)-oxomethyl]phenoxy]ethyl]-2-benzofurancarboxamide is a member of benzofurans. | [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. | [target]
HDAC1 | [storage]
Store at -20°C,unstable in solution, ready to use. | [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.. |
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