China (Mainland)
Enzalutamide (MDV3100) CAS NO.915087-33-1
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- Product Details
Keywords
- Enzalutamide
- MDV3100
- 915087-33-1
Quick Details
- ProName: Enzalutamide (MDV3100)
- CasNo: 915087-33-1
- Molecular Formula: C21H16F4N4O2S
- ProductionCapacity: Metric Ton/Day
- Purity: >97%
- LimitNum: 0 Metric Ton
Superiority
Biological Activity
| Description | Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy. | ||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| In vivo | Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1] |