726169-73-9 Mocetinostat AKSci X7532
 
 
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  X7532    AKSci Reference Standard
Mocetinostat, 99% (HPLC)
 
MGCD0103
IDENTITY
CAS Number:726169-73-9
MDL Number:MFCD10565970
MF:C23H20N6O
MW:396.44
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:99% (HPLC)
Physical Form (at 20°C):Solid
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO, Ethanol
Application(s):HDAC inhibitor for HDAC1, HDAC2 and HDAC3
Form:Free Base
Research Area:Cancer

REVIEW
 Mocetinostat (MGCD0103) is a potent benzamide histone deacetylase inhibitor with most potency for HDAC1 with IC50 of 0.15 µM, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinosta significantly inhibites growth of human tumor xenografts in nude mice and the antitumor activity correlated with induction of histone acetylation in tumors. MGCD0103 reduces pulmonary arterial pressure more dramatically than tadalafil, a standard-of-care therapy for human pulmonary hypertension that functions as a vasodilator. Moreover, MGCD0103 improves pulmonary artery acceleration time and reduced systolic notching of the pulmonary artery flow envelope, which suggests a positive impact of the HDAC inhibitor on pulmonary vascular remodeling and stiffening Mocetinostat is currently undergoing clinical trials for treatment of various cancers including follicular lymphoma, Hodgkin's lymphoma and acute myelogenous leukemia.

REFERENCES
[1]K. Gelmon, A. Tolcher, M. Carducci, G. K. Reid, Z. Li, A. Kalita, V. Callejas, J. Longstreth, J. M. Besterman and L. L. Siu Phase I trials of the oral histone deacetylase (HDAC) inhibitor MGCD0103 given either daily or 3x weekly for 14 days every 3 weeks in patients (pts) with advanced solid tumors Journal of Clinical Oncology, 2005 ASCO Annual Meeting Proceedings. Vol 23, No 16S (June 1 Supplement), 2005: 3147.
[2] Drug evaluation: MGCD-0103, a histone deacetylase inhibitor for the treatment of cancer. Kell J. Curr Opin Investig Drugs. 2007 Jun;8(6):485-92.
[3] Paquin I, Raeppel S, Leit S, Gaudette F, Zhou N, Moradei O, Saavedra O, Bernstein N, Raeppel F, Bouchain G, Fréchette S, Woo SH, Vaisburg A, Fournel M, Kalita A, Robert MF, Lu A, Trachy-Bourget MC, Yan PT, Liu J, Rahil J, MacLeod AR, Besterman JM, Li Z, Delorme D, Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1067-71.
[4] Le Tourneau C, Siu LL. Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor. Expert Opin Investig Drugs. 2008 Aug;17(8):1247-54.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501

Current as of April 19, 2024

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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