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

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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). 9/30/2014

   

MedKoo Cat#: 202170

Name: 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
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 purity > 98%, is available through custom synthesis. Minimum 1 gram order is requested. Current shipping out time is about 70 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 / Not Available

25mg / Not Available

50mg / Not Available

100mg / Not Available

200mg / Not Available

500mg / Not Available

1.0g / Ask price

2.0g / Ask price

5.0g / Ask price

Please ask price and availability of other quantity.

 

    

Technical data

Appearance:

white solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View current batch of CoA

QC data:

View NMR, View HPLC, View MS

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: 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.

2: Chalret du Rieu Q, Fouliard S, White-Koning M, Kloos I, Chatelut E, Chenel M. Pharmacokinetic/Pharmacodynamic modeling of abexinostat-induced thrombocytopenia across different patient populations: application for the determination of the maximum tolerated doses in both lymphoma and solid tumour patients. Invest New Drugs. 2014 Oct;32(5):985-94. doi: 10.1007/s10637-014-0118-1. Epub 2014 May 31. PubMed PMID: 24875134.

3: Gressette M, Vérillaud B, Jimenez-Pailhès AS, Lelièvre H, Lo KW, Ferrand FR, Gattolliat CH, Jacquet-Bescond A, Kraus-Berthier L, Depil S, Busson P. Treatment of nasopharyngeal carcinoma cells with the histone-deacetylase inhibitor abexinostat: cooperative effects with cis-platin and radiotherapy on patient-derived xenografts. PLoS One. 2014 Mar 11;9(3):e91325. doi: 10.1371/journal.pone.0091325. eCollection 2014. PubMed PMID: 24618637; PubMed Central PMCID: PMC3949989.

4: Bhalla S, Evens AM, Prachand S, Schumacker PT, Gordon LI. Paradoxical regulation of hypoxia inducible factor-1α (HIF-1α) by histone deacetylase inhibitor in diffuse large B-cell lymphoma. PLoS One. 2013 Nov 27;8(11):e81333. doi: 10.1371/journal.pone.0081333. eCollection 2013. PubMed PMID: 24312289; PubMed Central PMCID: PMC3842257.

5: Salvador MA, Wicinski J, Cabaud O, Toiron Y, Finetti P, Josselin E, Lelièvre H, Kraus-Berthier L, Depil S, Bertucci F, Collette Y, Birnbaum D, Charafe-Jauffret E, Ginestier C. The histone deacetylase inhibitor abexinostat induces cancer stem cells differentiation in breast cancer with low Xist expression. Clin Cancer Res. 2013 Dec 1;19(23):6520-31. doi: 10.1158/1078-0432.CCR-13-0877. Epub 2013 Oct 18. PubMed PMID: 24141629.

6: 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.

7: Rajak H, Singh A, Raghuwanshi K, Kumar R, Dewangan PK, Veerasamy R, Sharma PC, Dixit A, Mishra P. A structural insight into hydroxamic acid based histone deacetylase inhibitors for the presence of anticancer activity. Curr Med Chem. 2014;21(23):2642-64. PubMed PMID: 23895688.

8: Ali A, Bluteau O, Messaoudi K, Palazzo A, Boukour S, Lordier L, Lecluse Y, Rameau P, Kraus-Berthier L, Jacquet-Bescond A, Lelièvre H, Depil S, Dessen P, Solary E, Raslova H, Vainchenker W, Plo I, Debili N. Thrombocytopenia induced by the histone deacetylase inhibitor abexinostat involves p53-dependent and -independent mechanisms. Cell Death Dis. 2013 Jul 25;4:e738. doi: 10.1038/cddis.2013.260. PubMed PMID: 23887629; PubMed Central PMCID: PMC3730430.

9: Thomas S, Thurn KT, Raha P, Chen S, Munster PN. Efficacy of histone deacetylase and estrogen receptor inhibition in breast cancer cells due to concerted down regulation of Akt. PLoS One. 2013 Jul 9;8(7):e68973. doi: 10.1371/journal.pone.0068973. Print 2013. PubMed PMID: 23874830; PubMed Central PMCID: PMC3711340.

10: 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.

 

 

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