MDV3100 (Enzalutamide)
Catalog No.: GC12385Purity:>99.50%Synonyms: Enzalutamide
MDV3100 (Enzalutamide) is an oral inhibitor of androgen receptor (AR) with an IC50 value of 36nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 915087-33-1
10mgIn Stock
$24.00
1
25mgIn Stock
$48.00
1
50mgIn Stock
$71.00
1
100mgIn Stock
$118.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mg | $24.00 | In Stock | 1 | |
| 25mg | $48.00 | In Stock | 1 | |
| 50mg | $71.00 | In Stock | 1 | |
| 100mg | $118.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
3 publicationsPublications from researchers using this productDescription
MDV3100 (Enzalutamide) is an oral inhibitor of androgen receptor (AR) with an IC50 value of 36nM[1]. MDV3100 blocks AR interaction, inhibits translocation of the AR to the nucleus, impairs AR binding to DNA, and inhibits coactivator recruitment and receptor-mediated DNA transcription[2]. MDV3100 has been widely used to induce mitochondrial autophagy and inhibit the proliferation of prostate cancer cells[3].
In vitro, MDV3100 treatment for 144 hours significantly inhibited the proliferation of CW22Rv1 cells, with an IC50 value of 9.7μM[4]. Treatment with 100µM MDV3100 for 48 hours significantly inhibited the growth of AR-positive LNCaP cells, inducing nuclear condensation and fragmentation of DNA[5]. Treatment with 10µM MDV3100 for 72 hours significantly reduced the migration ability of MDA-MB-453 cells and downregulated the transcription factors AP-1 and SP-1[6].
In vivo, MDV3100 treatment via oral administration at a dose of 100mg/kg/day for 21 days reduced bone mass in the axial skeleton of male mice[7]. Oral administration of MDV3100 at a dose of 100mg/kg daily for 28 days reduced the tumor volume of LNCaP-AR xenograft tumors in mice and induced apoptosis of tumor cells[8].
References:
[1] Tran C, Ouk S, Clegg N J, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer[J]. Science, 2009, 324(5928): 787-790.
[2] Hoffman-Censits J, Kelly W K. Enzalutamide: a novel antiandrogen for patients with castrate-resistant prostate cancer[J]. Clinical Cancer Research, 2013, 19(6): 1335-1339.
[3] Han J, Zhang J, Zhang W, et al. Abiraterone and MDV3100 inhibits the proliferation and promotes the apoptosis of prostate cancer cells through mitophagy[J]. Cancer Cell International, 2019, 19(1): 332.
[4] Guerrini A, Tesei A, Ferroni C, et al. A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides[J]. Journal of Medicinal Chemistry, 2014, 57(17): 7263-7279.
[5] Abazid A, Martin B, Choinowski A, et al. The androgen receptor antagonist enzalutamide induces apoptosis, dysregulates the heat shock protein system, and diminishes the androgen receptor and estrogen receptor β1 expression in prostate cancer cells[J]. Journal of cellular biochemistry, 2019, 120(10): 16711-16722.
[6] Caiazza F, Murray A, Madden S F, et al. Preclinical evaluation of the AR inhibitor enzalutamide in triple-negative breast cancer cells[J]. Endocrine-related cancer, 2016, 23(4): 323-334.
[7] Wu J, Moverare-Skrtic S, Börjesson A E, et al. Enzalutamide reduces the bone mass in the axial but not the appendicular skeleton in male mice[J]. Endocrinology, 2016, 157(2): 969-977.
[8] Guerrero J, Alfaro I E, Gómez F, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration‐resistant prostate cancer[J]. The Prostate, 2013, 73(12): 1291-1305.
Protocol
| Cell experiment [1]: | |
|
Cell lines |
CW22Rv1 cells |
|
Preparation Method |
CW22Rv1 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS), and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. CW22Rv1 cells were seeded onto 96-well microplates (5×103 cells/well) and cultured for 24h. Cells were treated with the different concentrations of MDV3100 (0, 0.5, 1, 5, 10, 50, and 100μM) for 144h, cell viability was assessed. |
|
Reaction Conditions |
0, 0.5, 1, 5, 10, 50, and 100μM; 144h |
|
Applications |
MDV3100 treatment decreased the cell viability of CW22Rv1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Male CB17SCID mice |
|
Preparation Method |
Male CB17SCID mice (6 weeks old) were housed under controlled temperature (21-23°C), humidity (30-35%) and light cycle (7:00 AM to 7:00 PM) and maintained on a standard rodent diet. LNCaP-AR cells were prepared by the addition of trypsin-EDTA, washed with medium, collected and resuspended at 2×107 cells/ml. Cell suspensions were diluted with Matrigel to 2×106 cells/0.2 ml and delivered subcutaneously in the suprascapular region of mice. Tumor growth was monitored to the volume of 100mm3 when treatment began (80 days). The observed rate of tumor take with LNCaP-AR cells is between 70% and 80%. Body weight and tumor volumes (width2×length/2) were measured two times per week with a digital caliper, and the average tumor volumes were determined. MDV3100 was diluted in Tween 80:PEG 400, and stored at 4°C until administration by oral gavage. Mice were treated daily for 28 consecutive days with 50mg/kg MDV3100, vehicle control, or 50mg/kg bicalutamide. |
|
Dosage form |
50mg/kg/day; 28 days; p.o. |
|
Applications |
MDV3100 treatment significantly reduced tumor volume of LNCaP-AR xenograft tumors in mice. |
References: [1] Guerrini A, Tesei A, Ferroni C, et al. A new avenue toward androgen receptor pan-antagonists: C2 sterically hindered substitution of hydroxy-propanamides[J]. Journal of Medicinal Chemistry, 2014, 57(17): 7263-7279. [2] Guerrero J, Alfaro I E, Gómez F, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration‐resistant prostate cancer[J]. The Prostate, 2013, 73(12): 1291-1305. | |
Product Documents
Purity:>99.50%Appearance:A solid
Biological Data
1 / 1
Chemical Properties
CAS No.
915087-33-1
Synonyms
Enzalutamide
Chemical Name
4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide
SMILES
CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
Molecular Formula
C21H16F4N4O2S
Molecular Weight
464.4
Solubility
≥ 23.22mg/mL in DMSO
Storage
Store at-20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
Review for MDV3100 (Enzalutamide)
Rating: 5
- 5 Star100%
- 4 Star0%
- 3 Star0%
- 2 Star0%
- 1 Star0%