Abexinostat - CAS 783355-60-2
Catalog number: 783355-60-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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.
Publictions citing BOC Sciences Products
  • >> More
white solid powder
CRA-024781; CRA 024781; CRA024781; PCI-24781; PCI24781; PCI 24781; Abexinostat.
1.Histone deacetylase inhibitor abexinostat affects chromatin organization and gene transcription in normal B cells and in mantle cell lymphoma.
Markozashvili D1, Pichugin A2, Barat A1, Camara-Clayette V3, Vasilyeva NV4, Lelièvre H5, Kraus-Berthier L5, Depil S5, Ribrag V3, Vassetzky Y6. Gene. 2016 Apr 15;580(2):134-43. doi: 10.1016/j.gene.2016.01.017. Epub 2016 Jan 13.
Mantle cell lymphoma (MCL) is a rare lymphoma caused by the t(11:14) juxtaposing the cyclin D1 (CCND1) locus on chromosome 11 and the immunoglobulin heavy chain (IgH) locus on chromosome 14. Several new treatments are proposed for MCL, including histone deacetylase inhibitors (HDACi). We have studied gene expression and chromatin organization in the translocated 11q13 locus in MCL cells as compared to lymphoblastoid cell lines as well as the effect of HDACi abexinostat on chromatin organization and gene expression in the 11q13 locus. We have identified a cluster of genes overexpressed in the translocation region on chromosome 11 in MCL cells. Abexinostat provokes a genome-wide disaggregation of heterochromatin. The genes upregulated after the t(11;14) translocation react to the HDACi treatment by increasing their expression, but their gene promoters do not show significant alterations in H3K9Ac and H3K9me2 levels in abexinostat-treated cells.
2.A Phase I/II Multicenter, Open-Label Study of the Oral Histone Deacetylase Inhibitor Abexinostat in Relapsed/Refractory Lymphoma.
Evens AM1, Balasubramanian S2, Vose JM3, Harb W4, Gordon LI5, Langdon R6, Sprague J7, Sirisawad M2, Mani C2, Yue J2, Luan Y2, Horton S2, Graef T2, Bartlett NL8. Clin Cancer Res. 2016 Mar 1;22(5):1059-66. doi: 10.1158/1078-0432.CCR-15-0624. Epub 2015 Oct 19.
PURPOSE: Additional targeted therapeutics are needed for the treatment of lymphoma. Abexinostat is an oral pan-histone deacetylase inhibitor (HDACi) displaying potent activity in preclinical models. We conducted a multicenter phase I/II study (N = 55) with single-agent abexinostat in relapsed/refractory lymphoma.
3.Phase 1 study of the oral histone deacetylase inhibitor abexinostat in patients with Hodgkin lymphoma, non-Hodgkin lymphoma, or chronic lymphocytic leukaemia.
Morschhauser F1, Terriou L, Coiffier B, Bachy E, Varga A, Kloos I, Lelièvre H, Sarry AL, Depil S, Ribrag V. Invest New Drugs. 2015 Apr;33(2):423-31. doi: 10.1007/s10637-015-0206-x. Epub 2015 Jan 21.
Background We determined the safety, pharmacokinetics, pharmacodynamics, and antitumour activity of abexinostat in B-cell lymphoma or chronic lymphocytic leukaemia. Patients and methods Thirty-five patients received oral abexinostat 30, 45, or 60 mg/m(2) bid in a 3 + 3 design in three 21-day schedules: 14 days on treatment in schedule 1 (D1-14); 10 days in schedule 2 (D1-5 and D8-12); and 12 days in schedule 3 (D1-4, D8-11, and D15-18). Safety, tumour response, plasma concentration, and histone H3 acetylation were measured. Results Two dose-limiting toxicities occurred in each schedule (one grade 3 febrile neutropenia; five grade 4 thrombocytopenia) at 60 mg/m(2) bid (maximal tolerated dose). The recommended dose was 45 mg/m(2) bid; schedule 1 was considered optimal. Non-haematological drug-related toxicities included grade 1 or 2 diarrhoea (43%), nausea (23%), and vomiting (11%); haematological toxicities included thrombocytopenia (31% grade 3, and 26% grade 4), which remained manageable and reversible on withdrawal.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related HDAC Products

CAS 537034-15-4 NKL-22

(CAS: 537034-15-4)

NKL-22 is a HDAC inhibitor with IC 50 value of 78 uM. It is a cell-permeable pimeloylanilide compound which acts as a FXN-(frataxin gene) specific HDAC inhibito...

CAS 128517-07-7 Romidepsin

(CAS: 128517-07-7)

Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM ...

CAS 404950-80-7 Panobinostat

(CAS: 404950-80-7)

Panobinostat is a cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), induci...

Givinostat hydrochloride
(CAS: 199657-29-9)

Givinostat hydrochloride is the hydrochloride salt form of Givinostat. Givinostat, also called as GVS or ITF2357, a potent HDAC inhibitor for Maize HD2 (IC50= 1...

CAS 864814-88-0 Resminostat

(CAS: 864814-88-0)

Resminostat is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs ...

CAS 1314891-22-9 TMP195

(CAS: 1314891-22-9)

TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor (IC50s= 59 nM, 60 nM, 26 nM and 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9 respectively), and ...

CAS 1236199-60-2 EDO-S101

(CAS: 1236199-60-2)

EDO-S101 is a pan HDAC inhibitor (IC50= 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3, respectively). EDO-S101 is a first-in-class fusion molecule that combines DNA...

CAS 20554-84-1 (-)-Parthenolide

(CAS: 20554-84-1)

(-)-Parthenolide is a sesquiterpene lactone which occurs naturally in the plant feverfew(Tanacetum parthenium) and also promotes the ubiquitination of MDM2 and ...

CAS 156-54-7 Sodium butyrate

Sodium butyrate
(CAS: 156-54-7)

Sodium butyrate is the sodium salt of butyric acid, used in the culture of mammalian cells.

CAS 99873-43-5 Droxinostat

(CAS: 99873-43-5)

Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8. Droxinostat shows comparable inhibition of HDAC6 and HDAC8 (IC50 = 2.47 and 1.46 μmol/L, respec...

CAS 149647-78-9 Vorinostat

(CAS: 149647-78-9)

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM.

CAS 497833-27-9 Givinostat

(CAS: 497833-27-9)

Givinostat (INN) or gavinostat, aslo known as ITF2357,  is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic...

CAS 910462-43-0 4SC-202

(CAS: 910462-43-0)

4SC-202 is a selective and potent, orallly available inhibitor of histone deacetylases (HDAC) specific for class 1 HDAC isoenzymes, with IC50 of 1.20 μM, 1.12 μ...

CAS 58880-19-6 Trichostatin A

Trichostatin A
(CAS: 58880-19-6)

Trichostatin A, also known as TSA, is a HDAC inhibitor. TSA inhibits the eukaryotic cell cycle during the beginning of the growth stage. TSA can be used to alte...

CAS 848354-66-5 PTACH

(CAS: 848354-66-5)

PTACH is a SAHA-based novel inhibitor of histone deacetylase (HDAC). It exerts potent growth inhibition against various human cancer cells, with EC50 values ran...

CAS 1440209-96-0 BRD73954

(CAS: 1440209-96-0)

BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

CAS 1206731-57-8 WT-161

(CAS: 1206731-57-8)

WT-161 is a potent and specific HDAC6 inhibitor (IC50= 0.40 nM). Consistent with WT-161 mediated hyperacetylation and inhibition of hsp90 chaperone function, tr...

CAS 1187075-34-8 Resminostat hydrochloride

Resminostat hydrochloride
(CAS: 1187075-34-8)

Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6. As an inhibitor of...

Tinostamustine Hydrochloride
(CAS: 1793059-58-1)

The hydrochloride salt form of Tinostamustine, a benzimidazol derivative, has been found to be a HDAC inhibitor and could probably be effective against sorts of...

(CAS: 1316215-12-9)

HDAC-IN-2, a selective HDAC inhibitor, has been found to probably restrain the transcription and division of tumor oncogene and could also lead to the apoptosis...

Chemical Structure

CAS 783355-60-2 Abexinostat

Quick Inquiry

Verification code

Featured Items