Enzalutamide

Catalog No.S1250 Batch:S125012

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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
Ethanol 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 582 publications

Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388] PubMed: 38262412
RNA-sequencing predicts a role of androgen receptor and aldehyde dehydrogenase 1A1 in osteosarcoma lung metastases [ Oncogene, 2024, 43(14):1007-1018] PubMed: 38361046
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
Gαi2 Protein Inhibition Blocks Chemotherapy- and Anti-Androgen-Induced Prostate Cancer Cell Migration [ Cancers (Basel), 2024, 16(2)296] PubMed: 38254786
MALAT1 promotes FOXA1 degradation by competitively binding to miR-216a-5p and enhancing neuroendocrine differentiation in prostate cancer [ Transl Oncol, 2024, 39:101807] PubMed: 38235618
Combined therapy targeting AR and EZH2 curbs castration-resistant prostate cancer enhancing anti-tumor T-cell response [ Epigenomics, 2024, 10.2217/epi-2023-0374] PubMed: 38530086
Plexin D1 emerges as a novel target in the development of neural lineage plasticity in treatment-resistant prostate cancer [ Res Sq, 2024, rs.3.rs-4095949] PubMed: 38585965
CPT1a regulates the delivery of extracellular fatty acids for cardiolipin turnover in prostate cancer cells. [ bioRxiv, 2024, 10.1101/2024.01.16.575611] PubMed: none
CDK12 Loss Promotes Prostate Cancer Development While Exposing Vulnerabilities to Paralog-Based Synthetic Lethality [ bioRxiv, 2024, 2024.03.20.585990] PubMed: 38562774

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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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