CRA-02478

ChemicalBook > CAS DataBase List > CRA-02478

Product Name: CRA-02478
CAS No.: 783355-60-2
Chemical Name: CRA-02478
Synonyms: CS-423;PCI-24781;CRA-02478;CRA 24781;CRA 024781;Abexinostat;PCI-24781, >=98%;PCI-24781;CRA-02478;CRA-02478 PCI-24781;PCI-24781(CRA-024781)
CBNumber: CB12501009
Molecular Formula: C21H23N3O5
Formula Weight: 397.42
MOL File: 783355-60-2.mol

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CRA-02478 Property

Melting point:: 198-202oC (dec.)
Density: 1.284
storage temp.: Refrigerator
solubility: DMSO (Slightly), Methanol (Slightly, Heated)
form: Solid
pka: 9.04±0.10(Predicted)
color: White

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 20059
Product name: PCI 24781
Purity: ≥95%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 20059
Product name: PCI 24781
Purity: ≥95%
Packaging: 5mg
Price: $100
Updated: 2024/03/01

Cayman Chemical

Product number: 20059
Product name: PCI 24781
Purity: ≥95%
Packaging: 10mg
Price: $169
Updated: 2024/03/01

Cayman Chemical

Product number: 20059
Product name: PCI 24781
Purity: ≥95%
Packaging: 25mg
Price: $381
Updated: 2024/03/01

Usbiological

Product number: 019151
Product name: PCI-24781
Packaging: 10mg
Price: $460
Updated: 2021/12/16

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CRA-02478 Chemical Properties,Usage,Production

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

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..

CRA-02478 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from CRA-02478 manufacturers

Career Henan Chemical Co

Product: CRA-02478 783355-60-2
Price: US $2.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: customsie
Release date: 2018-08-20

783355-60-2, CRA-02478Related Search:

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CRA 024781

CRA 24781

CRA-02478

PCI-24781

PCI-24781(CRA-024781)

PCI-24781;CRA-02478

3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide

3-((diMethylaMino)Methyl)-N-(2-(4-(hydroxycarbaMoyl)phenoxy)ethyl)benzofuran-2-carboxaMide

CRA-02478 PCI-24781

PCI-24781 (Abexinostat)

Abexinostat

3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide PCI-24781

Abexinostat(PCI-24781)

2-Benzofurancarboxamide, 3-[(dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-

PCI-24781, >=98%

PCI-24781 (ABEXINOSTAT);PCI 24781

CRA-024781; CRA 024781; CRA024781; PCI24781; PCI-24781; PCI 24781; ABEXINOSTAT.

CS-423

CRA 024781;CRA 24781;PCI 24781;ABEXINOSTAT

3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide

CRA 024781;CRA 24781;ABEXINOSTAT

TIANFU CHEM---CRA-02478

Abexinostat (CRA 024781

Abexinostat CRA-024781 CRA024781

Abexinostat, 10 mM in DMSO

783355-60-2

Amines

Aromatics

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals

Inhibitor