LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase (HDAC) inhibitor with an IC50 of 0.032 μM. NVP-LAQ824 also inhibited patient MM cell growth in a dose- and time-dependent manner. NVP-LAQ824-induced apoptotic signaling includes up-regulation of p21, caspase cascade activation, and poly (adenosine diphosphate [ADP]) ribose (PARP) cleavage.
| Cell Experiment | |
|---|---|
| Cell lines | HCT116, H1299, PC-3, DU145 and MDA435 cells |
| Preparation method | Monolayer Growth Inhibition Assay. Cell proliferation was measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay) as described previously (29) . The CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay was performed according to the manufacturer’s protocol. The average background value (treatment with medium alone) was subtracted from each experimental well; triplicate values were averaged for each compound dilution. The following formulas were used to calculate the percentage of growth: The “% Growth” was plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition. |
| Concentrations | 0~10 μM |
| Incubation time | 72 hr |
| Animal Experiment | |
|---|---|
| Animal models | HCT116 cells tumor-bearing mice |
| Formulation | dissolved in DMSO to create a stock solution, which was further diluted just before dosing with D5W to a final DMSO concentration of 10%. |
| Dosages | once daily, 5 days/week, for a total of 15 doses. |
| Administration | i.v. injection into the tail vein |
| Molecular Weight | 379.459 |
| Formula | C22H25N3O3 |
| CAS Number | 404951-53-7 |
| Solubility (25°C) | DMSO |
| 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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