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Mocetinostat (MGCD0103, MG0103)
HDAC inhibitor,isotype-selective and potent

Mocetinostat (MGCD0103, MG0103)

Catalog No. A4089
Size Price Stock Qty
10mM (in 1mL DMSO) $130.00 In stock
Evaluation Sample $28.00 In stock
5mg $120.00 In stock
10mg $190.00 In stock
25mg $330.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

Mocetinostat (MGCD0103, MG0103)

Related Biological Data

Mocetinostat (MGCD0103, MG0103)

Related Biological Data

Mocetinostat (MGCD0103, MG0103)

Biological Activity

Description Mocetinostat (MGCD0103) is a potent inhibitor of HDAC 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.
Targets HDAC1 HDAC2 HDAC3      
IC50 0.15 μM 0.29 μM 1.66 μM      

Protocol

Cell experiment: [1]

Cell lines

A549 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

50 μM, 16 hours

Applications

MGCD0103 showed dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, MGCD0103 inhibited a maximum of 80% of total activity. Cells were then subsequently washed with drug-free media. The inhibitory activity of MGCD0103 was sustained at least 48 hours after drug removal followed by a slow reversal.

Animal experiment: [1]

Animal models

Female CD-1 nude mice injected with A549 cells

Dosage form

Oral administration, 120 mg/kg

Application

Administration of MGCD0103 (2HBr salt) significantly reduced growth of implanted advanced A549 tumors in nudemice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocked growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 did not reduce WBC counts and was well tolerated.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Fournel M, Bonfils C, Hou Y, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics, 2008, 7(4): 759-768.

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Chemical Properties

Cas No. 726169-73-9 SDF Download SDF
Synonyms MGCD-0103
Chemical Name N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide
Canonical SMILES C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
Formula C23H20N6O M.Wt 396.44
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Research Update

1. Mocetinostat for relapsed classical Hodgkin's lymphoma: an open-label, single-arm, phase 2 trial. Lancet Oncol. 2011 Dec;12(13):1222-8. doi: 10.1016/S1470-2045(11)70265-0. Epub 2011 Oct 25.
Abstract
Mocetinostat, a histone deacetylase inhibitor, has been assessed for safety and efficacy in patients with relapsed classical Hodgkin’s lymphoma.
2. Mocetinostat (MGCD0103): a review of an isotype-specific histone deacetylase inhibitor. Expert Opin Investig Drugs. 2011 Jun;20(6):823-9. doi: 10.1517/13543784.2011.577737. Epub 2011 May 10.
Abstract
HDACIs can be incorporated into treatments of lymphoma, myeloid leukemias and solid tumors for their potential to restore gene expression and display antitumor activity.

Background

Mocetinostat, also known as MGCD0103 or MG0103, is an isotype-selective inhibitor of human histone deacetylases (HDAC), a family of enzymes involved in epigenetic regulation of gene transcription as well as cell proliferation, death and motility. Mocetinostat potently inhibits HDAC class I (HDAC1, HDAC2, and HDAC3) and class IV (HDAC11), with values of inhibition constant IC50 of 0.15 μmol/L, 0.29 μmol/L, 1.66 μmol/L, and 0.59 μmol/L respectively, rather than HDAC class II. Mocetinostat exerts anti-tumor activity against a broad range of human cancer cells through HDAC inhibition, in which it induces histone hyperacetylation and apoptosis and causes cell cycle blockade in a dose-dependent manner.

Reference

Fournel M, Bonfils C, Hou Y, Yan PT, Trachy-Bourget MC, Kalita A, Liu J, Lu AH, Zhou NZ, Robert MF, Gillespie J, Wang JJ, Ste-Croix H, Rahil J, Lefebvre S, Moradei O, Delorme D, Macleod AR, Besterman JM, Li Z. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008; 7(4): 759-768