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MGCD0103

Cat. No. M1790

MGCD0103 Structure

Synonym: Mocetinostat

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 120 In stock
50mg USD 300 In stock
100mg USD 450 In stock
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Quality Control
Biological Activity

MGCD0103 (Mocetinostat) is a novel HDAC inhibitor, highly specific for classes I and IV HDACs. It is well-tolerated and exhibits favorable pharmacokinetic and pharmacodynamic profiles, demonstrating target inhibition and clinical responses. MGCD0103 (Mocetinostat) has been recently shown to exhibit various effects on non-histone targets on cancer cells. The latest preclinical studies have demonstrated that MGCD0103 can induce both cell death and autophagy.

Protocol
Cell Experiment
Cell lines HCT116, HCT15, HT29, DU145, MDA-mb231, A549 cells line
Preparation method Cell Viability Assay
Cells in 96-well plates were incubated with compounds at various concentrations for 72 h at 37°C in 5% CO2. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT; Sigma) was added at a final concentration of 0.5 mg/mL and incubated with the cells for 4 h before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] was added. After overnight incubation, solubilized dye was quantified by reading at 570 nm using a reference at 630 nm. Absorbance values were converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduced cell numbers to 50% relative to DMSO-treated cells was determined as MTT IC50.
Concentrations 0~100 μ M
Incubation time 72 h
Animal Experiment
Animal models Female CD-1 nude mice
Formulation PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60
Dosages daily for at least 2 weeks
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 396.44
Formula C23H20N6O
CAS Number 726169-73-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

Mocetinostat (MGCD0103): a review of an isotype-specific histone deacetylase inhibitor.
Boumber Y, et al. Expert Opin Investig Drugs. 2011 Jun;20(6):823-9. PMID: 21554162.

Histone deacetylase inhibitor MGCD0103 synergizes with gemcitabine in human pancreatic cells.
Sung V, et al. Cancer Sci. 2011 Jun;102(6):1201-7. PMID: 21375679.

The class I HDAC inhibitor MGCD0103 induces cell cycle arrest and apoptosis in colon cancer initiating cells by upregulating Dickkopf-1 and non-canonical Wnt signaling.
Sikandar S, et al. Oncotarget. 2010 Nov;1(7):596-605. PMID: 21317455.

Epigenetic modulation of MAGE-A3 antigen expression in multiple myeloma following treatment with the demethylation agent 5-azacitidine and the histone deacetlyase inhibitor MGCD0103.
Moreno-Bost A, et al. Cytotherapy. 2011 May;13(5):618-28. PMID: 21171821.

The class-I HDAC inhibitor MGCD0103 induces apoptosis in Hodgkin lymphoma cell lines and synergizes with proteasome inhibitors by an HDAC6-independent mechanism.
Buglio D, et al. Br J Haematol. 2010 Nov;151(4):387-96. PMID: 20880107.

The histone deacetylase inhibitor MGCD0103 has both deacetylase and microtubule inhibitory activity.
Chia K, et al. Mol Pharmacol. 2010 Sep;78(3):436-43. PMID: 20538840.

MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo.
Fournel M, et al. Mol Cancer Ther. 2008 Apr;7(4):759-68. PMID: 18413790.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MGCD0103, Mocetinostat supplier, HDAC, inhibitors

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