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.
Cell Experiment | |
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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 | |
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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. |
Molecular Weight | 396.44 |
Formula | C23H20N6O |
CAS Number | 726169-73-9 |
Solubility (25°C) | DMSO 20 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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