Enzalutamide
CAS No. : 915087-33-1
(Synonyms: MDV3100)
| Size | Price | Stock |
|---|---|---|
| 5mg | $50 | In-stock |
| 10mg | $70 | In-stock |
| 25mg | $95 | In-stock |
| 50mg | $120 | In-stock |
| 100mg | $190 | In-stock |
| 200mg | $240 | In-stock |
| 500mg | $350 | In-stock |
| 1g | $540 | In-stock |
| 2g | $730 | In-stock |
| 5g | $1180 | In-stock |
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| Cat. No. : | HY-70002 |
| M.Wt: | 464.44 |
| Formula: | C21H16F4N4O2S |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 50 mg/mL |
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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