Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by down-regulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). Droxinostat also downregulated c-FLIP expression, induced caspase-8- and caspase-3/7-mediated apoptosis, and increased apoptosis in bicalutamide-treated cells. Droxinostat shows a significant action on gene transcription hence controlling tumor progression. Droxinostat (10 μM - 100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis in MCF-7 breast cancer cells. In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.
| Cell Experiment | |
|---|---|
| Cell lines | PPC-1 cells |
| Preparation method | Viability of PPC-1 cells treated with 5809354 or 7271570 (0, 20, 40, 60, and 80 μM) with and without CH-11 (100 ng/mL) or cultured under adherent or suspension conditions and MEFs treated with 5809354 (0, 20, 40, 60, and 80 μM) under adherent or suspension conditions was assessed using the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium inner salt reduction assay (Promega, Madison, WI) according to the manufacturer's protocols as previous described (18). The percent relative cell viability was expressed as (optical density of treated cells/optical density of controls) × 100%. Two independent experiments were performed in triplicate (n = 6). |
| Concentrations | 0, 20, 40, 60, and 80 μM |
| Incubation time | 30 h |
| Animal Experiment | |
|---|---|
| Animal models | male SCID mice between 5 and 7 weeks of age prostate cancer cells in vivo |
| Formulation | PBS |
| Dosages | 30 μM |
| Administration | i.p. |
| Molecular Weight | 243.69 |
| Formula | C11H14ClNO3 |
| CAS Number | 99873-43-5 |
| Solubility (25°C) | DMSO 40 mg/mL Ethanol 40 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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