Enzalutamide [915087-33-1]

Catalog number: HY-70002_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 217.00
Expected delivery time: 10 days

Product specifications for - Enzalutamide [915087-33-1]

Product group: Chemicals
Category: Other
CAS No.: 915087-33-1
Purity: >98%
Molecular Formula: C21H16F4N4O2S
Molecular weight: 464.44
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM. IC50 value: 36 nM [1] Target: androgen-receptor in vitro: Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16beta-[18F]fluoro-5alpha-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].
Safety information: 
Anti-Androgen Abiraterone Acetate Improves the Therapeutic Efficacy of Statins on Castration-Resistant Prostate Cancer Cells', Dannah R. Miller. J Oncol Res Ther.20 December, 2017. Read more
SOCS3 Modulates the Response to Enzalutamide and is Regulated by AR Signaling and CpG Methylation in Prostate Cancer Cells', Handle F. Mol Cancer Res. 2016 Jun;14(6):574-85. Read more
Generation of a C57BL/6 MYC-driven mouse model and cell line of prostate cancer', Ellis L. Prostate. 2016 Sep;76(13):1192-202. Read more
Cellular androgen content influences enzalutamide agonism of F877L mutant androgen receptor', Coleman DJ. Oncotarget. 2016 Jun 28;7(26):40690-40703. Read more
Co-targeting HSP90 and its client proteins for treatment of prostate cancer', Long Chen. Mol Cancer Ther. 2016 Sep;15(9):2107-18. Read more
Critical role of androgen receptor level in prostate cancer cell resistance to new generation antiandrogen enzalutamide', Hoefer J. Oncotarget. 2016 Sep 13;7(37):59781-59794. Read more
Cancer-Associated Fibroblasts Modify the Response of Prostate Cancer Cells to Androgen and Anti-Androgens in Three-Dimensional Spheroid Culture.', Eder T. Int J Mol Sci. 2016 Sep 1;17(9). pii: E1458. Read more
Enzalutamide inhibits proliferation of gemcitabine-resistant bladder cancer cells with increased androgen receptor expression.', Koji Kameyama. Int J Oncol. 2017 Jan;50(1):75-84. Read more
Androgen Signaling in Esophageal Adenocarcinoma Cell Lines In Vitro', Palethorpe HM. Dig Dis Sci. 2017 Dec;62(12):3402-3414. Read more
Integrative molecular network analysis identifies emergent enzalutamide resistance mechanisms in prostate cancer', King CJ. Oncotarget. 2017 Nov 20;8(67):111084-111095. Read more