Abexinostat - CAS 783355-60-2
Catalog number: 783355-60-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H23N3O5
Molecular Weight:
397.431
COA:
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Targets:
HDAC
Description:
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.
Purity:
0.98
Appearance:
white solid powder
Synonyms:
CRA-024781; CRA 024781; CRA024781; PCI-24781; PCI24781; PCI 24781; Abexinostat.
MSDS:
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InChIKey:
MAUCONCHVWBMHK-UHFFFAOYSA-N
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)
Canonical SMILES:
CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
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.
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CAS 783355-60-2 Abexinostat

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