Enzalutamide
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CAS No. | 915087-33-1 | Cat. No. | BCP02361 |
Name | Enzalutamide | ||
Synonyms | MDV-3100;MDV3100;MDV 3100; | ||
SMILES | O=C(NC)C1=CC=C(N(C(N2C3=CC=C(C#N)C(C(F)(F)F)=C3)=S)C(C)(C)C2=O)C=C1F | ||
Chemical Name | |||
Formula | C21H16F4N4O2S | M. Wt | 464.44 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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).Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. |
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