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
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
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.
N-Bromosuccinimide Price
- Product number
- 20059
- Product name
- PCI 24781
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 20059
- Product name
- PCI 24781
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 20059
- Product name
- PCI 24781
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
- Product number
- 20059
- Product name
- PCI 24781
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $381
- Updated
- 2024/03/01
- Product number
- 019151
- Product name
- PCI-24781
- Packaging
- 10mg
- Price
- $460
- Updated
- 2021/12/16
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
- Product
- CRA-02478 783355-60-2
- Price
- US $2.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- customsie
- Release date
- 2018-08-20