MDV3100 (Enzalutamide)

Catalog No.S1250 Batch:S125014

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Technical Data

Formula

C21H16F4N4O2S
Molecular Weight 464.44 CAS No. 915087-33-1
Solubility (25°C)* In vitro DMSO 92 mg/mL (198.08 mM)
Water Insoluble
 
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Targets
Androgen Receptor [1]
(LNCaP cells)
36 nM
In vitro Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While this compound shows no agonism in LNCaP/AR prostate cells. It antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. This chemical could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). It also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.
In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.

Protocol (from reference)

Kinase Assay:[3]
  • AR reporter assay

    Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of this compound is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to this compound treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of this chemical. After two days of incubation, reporter activities are assayed.
Cell Assay:[1]
  • Cell lines

    LNCaP or LNCaP/AR cells

  • Concentrations

    0-10 μM

  • Incubation Time

    1-4 days

  • Method

    Enzalutamide is diluted in DMSO. LNCaP or LNCaP/AR cells (104 cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of this compound in media containing 5-10% charcoal-stripped serum.
Animal Study:[1]
  • Animal Models

    Castration-resistant LNCaP/HR xenografts in male SCID mice

  • Dosages

    10 mg/kg

  • Administration

    Administered via gavage daily

References

  • https://pubmed.ncbi.nlm.nih.gov/19359544/
  • https://pubmed.ncbi.nlm.nih.gov/20398925/
  • http://worldwide.espacenet.com/publicationDetails/originalDocument?CC=US&NR=2007254933A1&KC=A1&FT=D&

Customer Product Validation

Data from [ Cancer Sci , 2013 , 104(8), 1027-32 ]

Data from [ PLoS One , 2013 , 8, e53701 ]

Data from [ PLoS One , 2013 , 8, e53701 ]

Survival of mice receiving daily vehicle or MDV3100 treatment and treated with the LHRH-Ant or vehicle (n=10 mice per group). Data combined from two independent experiments.

Data from [ , , Nat Med, 2018, 24(2):239-246 ]

Selleck's MDV3100 (Enzalutamide) Has Been Cited by 585 Publications

Drugging the intrinsically disordered transactivation domain of androgen receptor [ Signal Transduct Target Ther, 2026, 11(1)157] PubMed: 42045150
TMEM121 suppresses cervical cancer cell proliferation and migration via interaction with the ERK pathway [ Am J Cancer Res, 2026, 16(1):70-87] PubMed: 41657789
OGDHL Promotes Prostate Cancer Progression and Regulates Neuroendocrine Marker Expression and Nucleotide Abundance [ Mol Cancer Res, 2026, 24(5):356-375] PubMed: 41591383
Synergistic roles of follicle-stimulating hormone and testosterone in Sertoli cell proliferation and testicular function in roosters [ Poult Sci, 2026, 105(3):106485] PubMed: 41576440
Identifying myosin heavy chain 11 as a predictive biomarker of prostate cancer progression and antiandrogen resistance [ Oncol Lett, 2026, 31(2):77] PubMed: 41467068
Circular RMST cooperates with lineage-driving transcription factors to govern neuroendocrine transdifferentiation [ Cancer Cell, 2025, 43(5):891-904.e10] PubMed: 40250444
Targeting histone H2B acetylated enhanceosomes via p300/CBP degradation in prostate cancer [ Nat Genet, 2025, 57(10):2468-2481] PubMed: 41044247
Genome-scale CRISPR screens identify PTGES3 as a direct modulator of androgen receptor function in advanced prostate cancer [ Nat Genet, 2025, 57(12):3027-3038] PubMed: 41193657
Off-pore nucleoporin sPOM121 transcriptionally propels β-Catenin driven tumor progression and immune escape in prostate cancer [ Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629] PubMed: 40709833
Engineering bi-directional chemically-modulated synthetic condensates for cellular control [ Nat Commun, 2025, 16(1):6587] PubMed: 40675979

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

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