Network Version
Enzalutamide Data Sheet
| Product Name: | Enzalutamide |
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| CAS No.: | 915087-33-1 | |
| Cat. No.: | HY-70002 | |
| MWt: | 464.44 | |
| Formula: | C21H16F4N4O2S | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 50 mg/mL | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator[1][2].
IC50 & Target:IC50: 36 nM (androgen-receptor, in LNCaP cells)[1]
In Vitro:Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 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 inhibits 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 (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg[1]. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg[4]. |
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