PCI-24781 (Abexinostat) - ≥97%, high purity , Histone deacetylase inhibitor, CAS No.783355-60-2, Histone deacetylase inhibitor

Item Number
P126975
Grouped product items
SKUSizeAvailabilityPrice Qty
P126975-1mg
1mg
In stock
$41.90
P126975-5mg
5mg
In stock
$90.90
P126975-10mg
10mg
In stock
$142.90
P126975-50mg
50mg
In stock
$456.90

Broad-spectrum histone deacytylase (HDAC) inhibitor.

Basic Description

SynonymsDB12565 | BDBM24622 | ABEXINOSTAT [WHO-DD] | AKOS025149423 | FT-0673532 | UDWXLZLRRVQONG-UHFFFAOYSA-M | CRA-02478 | Abexinostat [USAN:INN] | SY035141 | 3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide | CCG-264
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsPCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar ran
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionHistone deacetylase inhibitor
NoteToxic, refer to SDS for further information . Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

PCI-24781 (Abexinostat) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.
An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor.

Product Properties

ALogP2.2

Associated Targets(Human)

HDAC4 Tclin Histone deacetylase 4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC6 Tclin Histone deacetylase 6 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC1 Tclin Histone deacetylase 1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC7 Tclin Histone deacetylase 7 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC11 Tclin Histone deacetylase 11 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC9 Tclin Histone deacetylase 9 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC2 Tclin Histone deacetylase 2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC10 Tclin Histone deacetylase 10 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC8 Tclin Histone deacetylase 8 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC5 Tclin Histone deacetylase 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HDAC3 Tclin Histone deacetylase 3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LTA4H Tchem Leukotriene A4 hydrolase (1442 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC8 Tclin Histone deacetylase 8 (4516 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC10 Tclin Histone deacetylase 10 (801 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC2 Tclin Histone deacetylase 2 (3971 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC3 Tclin Histone deacetylase 3 (3654 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC4 Tclin Histone deacetylase 4 (2328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC9 Tclin Histone deacetylase 9 (708 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC11 Tclin Histone deacetylase 11 (967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC7 Tclin Histone deacetylase 7 (1047 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HDAC3 Tclin Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (735 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac1 Histone deacetylase 1 (93 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac5 Histone deacetylase 5 (5 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trypanosoma brucei brucei (13300 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Schistosoma mansoni (6170 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide
INCHI InChI=1S/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)
InChi Key MAUCONCHVWBMHK-UHFFFAOYSA-N
Canonical SMILES CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
Isomeric SMILES CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
PubChem CID 11749858
Molecular Weight 397.42

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

4 results found

Lot NumberCertificate TypeDateItem
I2214766Certificate of AnalysisJun 19, 2024 P126975
I2214767Certificate of AnalysisJun 19, 2024 P126975
I2214768Certificate of AnalysisJun 19, 2024 P126975
I2214769Certificate of AnalysisJun 19, 2024 P126975

Chemical and Physical Properties

SolubilityDMSO ≥78mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Safety and Hazards(GHS)

Pictogram(s) GHS06,   GHS08,   GHS09,   GHS05,   GHS07
Signal Danger
Hazard Statements

H311:Toxic in contact with skin

H373:Causes damage to organs through prolonged or repeated exposure

H411:Toxic to aquatic life with long lasting effects

H314:Causes severe skin burns and eye damage

H302:Harmful if swallowed

H318:Causes serious eye damage

H361:Suspected of damaging fertility or the unborn child

Precautionary Statements

P273:Avoid release to the environment.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P270:Do not eat, drink or smoke when using this product.

P301+P330+P331:IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.

P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing.

P363:Wash contaminated clothing before reuse.

P391:Collect spillage.

P330:Rinse mouth.

P361+P364:Take off immediately all contaminated clothing and wash it before reuse.

P203:Obtain, read and follow all safety instructions before use.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P301+P317:IF SWALLOWED: Get medical help.

P305+P354+P338:IF IN EYES: Immediately rinse with water for several minutes. Remove contact lenses if present and easy to do. Continue rinsing.

P318:if exposed or concerned, get medical advice.

P317:Get emergency medical help.

P302+P361+P354:IF ON SKIN: Take off Immediately all contaminated clothing. Immediately rinse with water for several minutes.

P316:Get emergency medical help immediately.

P319:Get medical help if you feel unwell.

Related Documents

References

1. Buggy JJ, Cao ZA, Bass KE, Verner E, Balasubramanian S, Liu L, Schultz BE, Young PR, Dalrymple SA.  (2006)  CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo..  Mol Cancer Ther,  (5): (1309-17).  [PMID:16731764] [10.1021/op500134e]
2. Liu L, Chen B, Qin S, Li S, He X, Qiu S, Zhao W, Zhao H.  (2010)  A novel histone deacetylase inhibitor Chidamide induces apoptosis of human colon cancer cells..  Biochem Biophys Res Commun,  392  (2): (190-5).  [PMID:20060381] [10.1021/op500134e]
3. Mithraprabhu S, Grigoriadis G, Khong T, Spencer A.  (2010)  Deactylase inhibition in myeloproliferative neoplasms..  Invest New Drugs,  28 Suppl 1  (13): (S50-7).  [PMID:21127942] [10.1021/op500134e]
4. Prebet T, Vey N.  (2011)  Vorinostat in acute myeloid leukemia and myelodysplastic syndromes..  Expert Opin Investig Drugs,  20  (2): (287-95).  [PMID:21192773] [10.1021/op500134e]

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