Enzalutamide

Catalog No.S1250 Batch:S125018

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Technical Data

Formula

C21H16F4N4O2S
Molecular Weight 464.44 CAS No. 915087-33-1
Solubility (25°C)* In vitro DMSO 93 mg/mL (200.24 mM)
Ethanol 4 mg/mL (8.61 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 613 publications

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
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388] PubMed: 38262412
PROX1 drives neuroendocrine plasticity and liver metastases in prostate cancer [ Cancer Lett, 2024, 597:217068] PubMed: 38901665
Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer [ Cancer Lett, 2024, 604:217219] PubMed: 39244005
Understanding the function of Pax5 in development of docetaxel-resistant neuroendocrine-like prostate cancers [ Cell Death Dis, 2024, 15(8):617] PubMed: 39183332
RNA-sequencing predicts a role of androgen receptor and aldehyde dehydrogenase 1A1 in osteosarcoma lung metastases [ Oncogene, 2024, 43(14):1007-1018] PubMed: 38361046
Oxidative stress in peroxisomes induced by androgen receptor inhibition through peroxisome proliferator-activated receptor promotes enzalutamide resistance in prostate cancer [ Free Radic Biol Med, 2024, 221:81-88] PubMed: 38762061
Upregulation of key factors of viral entry of corona- and influenza viruses upon TLR3-signaling in cells from the respiratory tract and clinical treatment options by 1,8-Cineol [ Phytother Res, 2024, 10.1002/ptr.8280] PubMed: 39020450
Manzamine A reduces androgen receptor transcription and synthesis by blocking E2F8-DNA interactions and effectively inhibits prostate tumor growth in mice [ Mol Oncol, 2024, 10.1002/1878-0261.13637] PubMed: 38605607
ST3 beta-galactoside alpha-2,3-sialyltransferase 1 (ST3Gal1) synthesis of Siglec ligands mediates anti-tumour immunity in prostate cancer [ Commun Biol, 2024, 7(1):276] PubMed: 38448753

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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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