. Abexinostat | PCI-24781(CRA-024781)| CAS#783355-60-2 | HDAC inhibitor | MedKoo Biosciences

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 PCI-24781(Abexinostat)

   

Description of Abexinostat: Abexinostat, also known as PCI-24781 or CRA-024781, is novel, broad-spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. Abexinostat inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis. HDAC, upregulated in many tumor types, is an an enzyme that is responsible for the deacetylation of chromatin histone proteins. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (last updated: 4/11/2015)

   

MedKoo Cat#: 202170

Name: PCI-24781 (Abexinostat)

CAS#: 783355-60-2

Synonym: CRA-024781; CRA 024781; CRA024781; PCI-24781; PCI24781; PCI 24781; Abexinostat.

IUPAC/Chemical name: 

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

Chemical structure:

Theoretical analysis:

 

MedKoo Cat#: 202170
Name:
PCI-24781 (Abexinostat)
CAS#: 783355-60-2

Chemical Formula: C21H23N3O5

Exact Mass: 397.16377

Molecular Weight: 397.42

Elemental Analysis: C, 63.46; H, 5.83; N, 10.57; O, 20.13

 

Availability and price:

Abexinostat (PCI24781); purity > 96%, is in stock. Price updated on 4/11/2015.  Current shipping out time is about 10 days after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee from: $30.00 (USA); $45.00 (Canada); $70.00 (international).

10mg / $90.00

25mg / $150.00

50mg / $250.00

100mg / $450.00

200mg / $850.00

500mg / $1,250.00

1.0g / $1,950.00

2.0g / $2,950.00

5.0g / Ask price

Please ask price and availability of other quantity.

  

    

Technical data

Appearance:

white to off-white solid powder

Purity:

>96% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View CoA: current batch, Lot#SSC50423

QC data:

View QC data: current batch, Lot#SSC50423

Safety Data Sheet (MSDS):

View Material Safety Data Sheet (MSDS)

Shipping condition:

Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage condition:

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:

Soluble in DMSO, not in water

Shelf life:

>2 years if stored properly

Drug formulation:

This drug may be formulated in DMSO

Stock solution storage:

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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Protocols from literature

In vitro protocol::

XXX

In vivo protocol:

XXX

Clinical study:

XXX

Review papers:

XXX

 

Information about this agent

 

References:

1: Correction: Combining PCI-24781, a Novel Histone Deacetylase Inhibitor, with Chemotherapy for the Treatment of Soft Tissue Sarcoma. Clin Cancer Res. 2015 Apr 1;21(7):1774-5. doi: 10.1158/1078-0432.CCR-15-0351. PubMed PMID: 25833311.

2: Sholler GS, Currier EA, Dutta A, Slavik MA, Illenye SA, Mendonca MC, Dragon J, Roberts SS, Bond JP. PCI-24781 (abexinostat), a novel histone deacetylase inhibitor, induces reactive oxygen species-dependent apoptosis and is synergistic with bortezomib in neuroblastoma. J Cancer Ther Res. 2013 Dec 28;2:21. PubMed PMID: 25520806; PubMed Central PMCID: PMC4266584.

3: Zhang W, Lv S, Liu J, Zang Z, Yin J, An N, Yang H, Song Y. PCI-24781 down-regulates EZH2 expression and then promotes glioma apoptosis by suppressing the PIK3K/Akt/mTOR pathway. Genet Mol Biol. 2014 Oct;37(4):716-24. doi: 10.1590/S1415-47572014005000011. Epub 2014 Oct 21. PubMed PMID: 25505847; PubMed Central PMCID: PMC4261972.

4: He WL, Li YH, Hou WJ, Ke ZF, Chen XL, Lu LY, Cai SR, Song W, Zhang CH, He YL. RAD51 potentiates synergistic effects of chemotherapy with PCI-24781 and cis-diamminedichloroplatinum on gastric cancer. World J Gastroenterol. 2014 Aug 7;20(29):10094-107. doi: 10.3748/wjg.v20.i29.10094. PubMed PMID: 25110436; PubMed Central PMCID: PMC4123338.

5: Zhan Q, Tsai S, Lu Y, Wang C, Kwan Y, Ngai S. RuvBL2 is involved in histone deacetylase inhibitor PCI-24781-induced cell death in SK-N-DZ neuroblastoma cells. PLoS One. 2013 Aug 16;8(8):e71663. doi: 10.1371/journal.pone.0071663. eCollection 2013. PubMed PMID: 23977108; PubMed Central PMCID: PMC3745445.

6: Fouliard S, Robert R, Jacquet-Bescond A, du Rieu QC, Balasubramanian S, Loury D, Loriot Y, Hollebecque A, Kloos I, Soria JC, Chenel M, Depil S. Pharmacokinetic/pharmacodynamic modelling-based optimisation of administration schedule for the histone deacetylase inhibitor abexinostat (S78454/PCI-24781) in phase I. Eur J Cancer. 2013 Sep;49(13):2791-7. doi: 10.1016/j.ejca.2013.05.009. Epub 2013 Jun 18. PubMed PMID: 23790467.

7: Chalret du Rieu Q, Fouliard S, Jacquet-Bescond A, Robert R, Kloos I, Depil S, Chatelut E, Chenel M. Application of hematological toxicity modeling in clinical development of abexinostat (S-78454, PCI-24781), a new histone deacetylase inhibitor. Pharm Res. 2013 Oct;30(10):2640-53. doi: 10.1007/s11095-013-1089-1. Epub 2013 Jun 5. PubMed PMID: 23737346.

8: Kitamura T, Connolly K, Ruffino L, Ajiki T, Lueckgen A, DiGiovanni J, Kiguchi K. The therapeutic effect of histone deacetylase inhibitor PCI-24781 on gallbladder carcinoma in BK5.erbB2 mice. J Hepatol. 2012 Jul;57(1):84-91. doi: 10.1016/j.jhep.2012.01.018. Epub 2012 Feb 9. PubMed PMID: 22326466; PubMed Central PMCID: PMC3378818.

9: Yang C, Choy E, Hornicek FJ, Wood KB, Schwab JH, Liu X, Mankin H, Duan Z. Histone deacetylase inhibitor PCI-24781 enhances chemotherapy-induced apoptosis in multidrug-resistant sarcoma cell lines. Anticancer Res. 2011 Apr;31(4):1115-23. PubMed PMID: 21508354; PubMed Central PMCID: PMC3744220.

10: Yang C, Choy E, Hornicek FJ, Wood KB, Schwab JH, Liu X, Mankin H, Duan Z. Histone deacetylase inhibitor (HDACI) PCI-24781 potentiates cytotoxic effects of doxorubicin in bone sarcoma cells. Cancer Chemother Pharmacol. 2011 Feb;67(2):439-46. doi: 10.1007/s00280-010-1344-7. Epub 2010 May 12. PubMed PMID: 20461381.

 

 

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