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Cat. No. M1839
MDV3100 Structure

Enzalutamide, MDV-3100

Size Price Availability Quantity
10mg USD 145 In stock
50mg USD 380 In stock
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Quality Control
Biological Activity

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.

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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 464.44
Formula C21H16F4N4O2S
CAS Number 915087-33-1
Purity 98.27%
Solubility DMSO ≥91 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
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
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.

Biomarker-based targeting of the androgen-androgen receptor axis in advanced prostate cancer.
Kohli et al. Adv Urol. 2012. PMID: 22956944.

Increased Survival with Enzalutamide in Prostate Cancer after Chemotherapy.
Scher et al. N Engl J Med. 2012 Aug 15. PMID: 22894553.

Abiraterone and other novel androgen-directed strategies for the treatment of prostate cancer: a new era of hormonal therapies is born.
Schweizer et al. Ther Adv Urol. 2012 Aug;4(4):167-78. PMID: 22852027.

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Keywords: MDV3100, Enzalutamide, MDV-3100 supplier, CYP17, inhibitors

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