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ARV-771 is a small-molecule pan-BET degrader with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively. ARV-771 potently degrades BRD2/3/4 in 22Rv1 cells with a DC50 less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC50 of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines.
In vivo, treatment of non castrated male Nu/Nu mice bearing AR-V7+ 22Rv1 tumor xenografts with daily subcutaneous injections of ARV-771 at 10 mg/kg for 3 d results in 37% and 76% down-regulation of BRD4 and c-MYC levels, respectively, in tumor tissue.
| Cell Experiment | |
|---|---|
| Cell lines | 22Rv1 cells |
| Preparation method | ARV-771 is dissolved in DMSO. 22Rv1 cells (5,000 cells per well) are dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h. CellTiter-Glo Luminescent Cell Viability Assay is added, and the plate is read on a luminometer. Data are analyzed and plotted using GraphPad Prism software. |
| Concentrations | |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing tumors |
| Formulation | |
| Dosages | (5, 10, 30, 50 mg/kg) for up to 3 wk |
| Administration | |
| Molecular Weight | 986.64 |
| Formula | C49H60ClN9O7S2 |
| CAS Number | 1949837-12-0 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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