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Mocetinostat (MGCD0103, MG0103)

HDAC inhibitor,isotype-selective and potent CAS# 726169-73-9

Mocetinostat (MGCD0103, MG0103)

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Chemical structure

Mocetinostat (MGCD0103, MG0103)

3D structure

Chemical Properties of Mocetinostat (MGCD0103, MG0103)

Cas No. 726169-73-9 SDF Download SDF
PubChem ID 9865515 Appearance Powder
Formula C23H20N6O M.Wt 396.44
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MGCD0103
Solubility DMSO : 50 mg/mL (126.12 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide
SMILES C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
Standard InChIKey HRNLUBSXIHFDHP-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29)
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Mocetinostat (MGCD0103, MG0103)

DescriptionMocetinostat (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.
TargetsHDAC1HDAC2HDAC3   
IC500.15 μM0.29 μM1.66 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.

Mocetinostat (MGCD0103, MG0103) Dilution Calculator

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Preparing Stock Solutions of Mocetinostat (MGCD0103, MG0103)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5224 mL 12.6122 mL 25.2245 mL 50.449 mL 63.0612 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL 10.0898 mL 12.6122 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 5.0449 mL 6.3061 mL
50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.009 mL 1.2612 mL
100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.5045 mL 0.6306 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Research Update of Mocetinostat (MGCD0103, MG0103)

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.

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Background on Mocetinostat (MGCD0103, MG0103)

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

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References on Mocetinostat (MGCD0103, MG0103)

Mocetinostat (MGCD0103): a review of an isotype-specific histone deacetylase inhibitor.[Pubmed:21554162]

Expert Opin Investig Drugs. 2011 Jun;20(6):823-9.

INTRODUCTION: HDAC inhibitors (HDACIs) have the potential to restore gene expression and display antitumor effects in vitro. As single agents, HDACIs have clinical activity in lymphoma. In myeloid leukemias, combinations of DNA methylation inhibitors and HDACIs are promising. Other combinations are being studied in solid tumors. AREAS COVERED: This article covers basic information and an update on preclinical and clinical experience with the oral isotype-selective HDACI MGCD0103 (mocetinostat) in hematological malignancies and solid tumors. It also examines data concerning MGCD0103 from recent conferences and articles through to November 2010, including new data regarding responses in lymphoma and toxicities. EXPERT OPINION: MGCD0103 is well-tolerated and exhibits favorable pharmacokinetic and pharmacodynamic profiles, demonstrating target inhibition and clinical responses. It induces cell death and autophagy, synergizes with proteasomal inhibitors and affects non-histone targets, such as microtubules. In 2008, new patient enrollment in trials was temporarily suspended due to potential cardiac complications. This restriction was lifted in 2009 as no correlation between MGCD0103 exposure and pericardial effusions was found. New patient enrollment in MGCD0103 clinical trials requires the exclusion of patients diagnosed with significant cardiac abnormalities prior to enrollment. Clinical and pharmacodynamic data support a three-times-weekly administration at a 90 mg fixed dose. MGCD0103 displays promising antitumor activity in several hematological diseases.

Liquid chromatography mass spectrometry determination of mocetinostat (MGCD0103) in rat plasma and its application to a pharmacokinetic study.[Pubmed:24588344]

Xenobiotica. 2014 Sep;44(9):849-54.

Mocetinostat (MGCD0103) is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers including Hodgkin's lymphoma, follicular lymphoma and acute myelogenous leukemia. A sensitive and selective liquid chromatography mass spectrometry method for determination of MGCD0103 in rat plasma was developed. After addition of midazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographic separation was achieved on a C18 (2.1 mmx50 mm, 3.5 microm) column with acetonitrile-0.1% formic acid in water as mobile phase with gradient elution. An electrospray ionization source was applied and operated in positive ion mode; selective ion monitoring (SIM) mode was used for quantification using target fragment ions m/z 397 for MGCD0103 and m/z 326 for the IS. Calibration plots were linear over the range of 5-5000 ng/mL for MGCD0103 in rat plasma. Mean recoveries of MGCD0103 in rat plasma were in the range of 89.7-96.1%. RSD of intra-day and inter-day precision were both<11%. The accuracy of the method ranged from 96.5% to 109.7%. The matrix effects for MGCD0103 were between 94.5% and 97.4%. The method was successfully applied to pharmacokinetic study of MGCD0103 after oral (15 mg/kg) and intravenous (3 mg/kg) administration in rats. The bioavailability of MGCD0103 was 29.3% in rats.

Metabolic changes in rats after intragastric administration of MGCD0103 (Mocetinostat), a HDAC class I inhibitor.[Pubmed:26464683]

Int J Clin Exp Pathol. 2015 Aug 1;8(8):9320-5. eCollection 2015.

MGCD0103, an isotype-selective HDACi, has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agents. In this study, we developed a serum metabolomic method based on gas chromatography-mass spectrometry (GC-MS) to evaluate the effect of intragastric administration of MGCD0103 on rats. The MGCD0103 group rats were given 20, 40, 80 mg/kg of MGCD0103 by intragastric administration each day for 7 days. Pattern recognition analysis, including both principal component analysis (PCA) and partial least squares-discriminate analysis (PLS-DA) revealed that intragastric administration of MGCD0103 induced metabolic perturbations. As compared to the control group, the levels of L-alanine, L-isoleucine, and L-leucine of MGCD0103 group decreased. The results indicate that metabolomic methods based on GC-MS may be useful to elucidate side effect of MGCD0103 through the exploration of biomarkers (L-alanine, L-isoleucine, and L-leucine). According to the pathological changes of liver at difference dosage, MGCD0103 is hepatotoxic and its toxity is dose-dependent.

Description

Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.

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