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
 
* <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.)

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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 Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2]
In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]

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 Enzalutamide 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 Enzalutamide 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 Enzalutamide. 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 Enzalutamide 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

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]

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

Selleck's Enzalutamide has been cited by 634 publications

An Autophagy-Targeting Chimera Induces Degradation of Androgen Receptor Mutants and AR-v7 in Castration-Resistant Prostate Cancer [ Cancer Res, 2025, 85(2):342-359] PubMed: 39531508
PlexinD1 is a driver and a therapeutic target in advanced prostate cancer [ EMBO Mol Med, 2025, 17(2):336-364] PubMed: 39748059
EHMT2-mediated R-loop formation promotes the malignant progression of prostate cancer via activating Aurora B [ Clin Transl Med, 2025, 15(1):e70164] PubMed: 39763034
Increased nuclear factor I-mediated chromatin access drives transition to androgen receptor splice variant dependence in prostate cancer [ Cell Rep, 2025, 44(1):115089] PubMed: 39709604
CRISPR screening identifies regulators of enhancer-mediated androgen receptor transcription in advanced prostate cancer [ Cell Rep, 2025, 44(2):115312] PubMed: 39954255
Mechanism of Action and Interaction of Garlic Extract and Established Therapeutics in Prostate Cancer [ Int J Mol Sci, 2025, 26(4)1777] PubMed: 40004239
Rapid and high-throughput screening of proteolysis targeting chimeras using a dual-reporter system expressing fluorescence protein and luciferase [ BMC Biol, 2025, 23(1):51] PubMed: 39985000
The Homeobox Transcription Factor NKX3.1 Displays an Oncogenic Role in Castration-Resistant Prostate Cancer Cells [ Cancers (Basel), 2025, 17(2)306] PubMed: 39858088
Increased translation driven by non-canonical EZH2 creates a synthetic vulnerability in enzalutamide-resistant prostate cancer [ Nat Commun, 2024, 15(1):9755] PubMed: 39567499
Precise nano-system-based drug delivery and synergistic therapy against androgen receptor-positive triple-negative breast cancer [ Acta Pharm Sin B, 2024, 14(6):2685-2697] PubMed: 38828153

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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.

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