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MDV3100 is an orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. MDV3100 (Enzalutamide) blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces tumour cell apoptosis, and has no agonist activity. Early preclinical studies also suggest that MDV3100 inhibits breast cancer cell growth.
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MDV3100 purchased from AbMole
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SMAD3 promotes expression and activity of the androgen receptor in prostate cancer
MDV3100 purchased from AbMole
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Source | Mol Cancer Ther (2013). Figure 2. MDV3100 |
| Method | Weatern Blot | |
| Cell Lines | LNCaP cells | |
| Concentrations | 0.01, 0.1, 1, 10, 100, 1000 μmol/L | |
| Incubation Time | 72 h | |
| Results | We further investigated the effects on cell-cycle progression by analyzing the expression of cyclin D protein, which is known as aG1 phase cyclin that regulates the entry of cells intoG1, in Compound 30- and MDV3100-treated tumors |
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Source | Mol Cancer Ther (2013). Figure 1. MDV3100 |
| Method | Weatern Blot | |
| Cell Lines | LNCaP cells | |
| Concentrations | 10 μmol/L | |
| Incubation Time | 24 h | |
| Results | We found that Compound 30 decreased AR transcriptional activity, measured by probasin luciferase activity (Fig. 1B, top left), in a dose-dependent manner and with greater potency compared with MDV3100 [probasin 50% effective concentration (EC50): 12.5 and 20 mmol/L, respectively. |
| Cell Experiment | |
|---|---|
| Cell lines | VCaP cell line |
| Preparation method | Proliferation assays Trypsinized VCaP cells were adjusted to a concentration of 100,000 cells per mL in phenol-red-free RPMI 1640 (with 5% CSS), and dispensed in 16 µL aliquots into CellBIND 384 well plates (Corning, Lowell, MA). Cells were incubated for 48 hours, after which ligand was added in a 16 µL volume to the RPMI culture medium. For the antagonist mode assay, the ligands were diluted in culture medium also containing 30 pM R1881 (final [R1881] = 15 pM). After 7 days’ incubation, 16 µL of CellTiter-Glo Luminescent Cell Viability Assay (Promega, Madison, WI) was added and Relative Luminescence Units (RLUs) measured. In the agonist mode assay, percent viability of the samples was calculated as: % viability=[RLU sample-RLU medium without cells]/[RLU DMSO treated cells-RLU medium without cells]. In the antagonist mode assay, the percent viability of the samples was calculated as: % viability=[RLU sample-RLU VCaP without R1881]/[RLU R1881-treated cells - RLU VCaP without R1881]. |
| Concentrations | 0~10µM |
| Incubation time | 48h |
| Animal Experiment | |
|---|---|
| Animal models | LNCaP/AR(cs) xenograft model in mice |
| Formulation | prepared in 18% PEG-400, 1% Tween-80 and 1% povidone, and were formulated for dosing in 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0). |
| Dosages | 100mg/kg |
| Administration | oral gavage |
| Molecular Weight | 464.44 |
| Formula | C21H16F4N4O2S |
| CAS Number | 915087-33-1 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Androgen Receptor Products |
|---|
| N-Desmethyl Enzalutamide
N- Desmethyl Enzalutamide |
| Norelgestromin
Norgestimate and its metabolite norelgestromin possess weak androgen-like properties. |
| Bicalutamide
Bicalutamide is an orally active non-steroidal androgen receptor antagonist (IC50 = 190 nM). |
| Ostarine
Ostarine (GTx-024 and MK-2866) is an investigational selective androgen receptor modulator (SARM) with Ki of 3.8 nM. |
| Andarine
Andarine (GTx-007, S-4) is a selective nonsteroidal androgen receptor (AR) agonist with Ki of 4 nM. |
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