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Enzalutamide (MDV3100)
Catalog No.S1250
For research use only.
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
CAS No. 915087-33-1
Selleck's Enzalutamide (MDV3100) has been cited by 418 publications
Purity & Quality Control
Choose Selective Androgen Receptor Inhibitors
Related Compound Libraries
Other Androgen Receptor Products
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] |
Protocol (from reference)
| Kinase Assay:[3] |
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| Cell Research:[1] |
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| Animal Research:[1] |
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 464.44 | ||
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| Formula | C21H16F4N4O2S |
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| CAS No. | 915087-33-1 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C | ||
In vivo Formulation Calculator (Clear solution)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05191017 | Not yet recruiting | Drug: NUV-422|Drug: Enzalutamide | Prostate Cancer|Prostatic Cancer|Cancer of Prostate|Cancer of the Prostate|Prostate Neoplasm|Castrate Resistant Prostate Cancer|Castration Resistant Prostatic Cancer|Castration Resistant Prostatic Neoplasms | Nuvation Bio Inc. | April 2022 | Phase 1|Phase 2 |
| NCT05081193 | Not yet recruiting | Drug: Testosterone Undecanoate|Drug: Enzalutamide | Prostate Cancer|Castration-resistant Prostate Cancer|Metastatic Castration-resistant Prostate Cancer | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Clarus Therapeutics | February 15 2022 | Phase 2 |
| NCT04335682 | Recruiting | Drug: Darolutamide|Drug: Enzalutamide | Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer | Alliance Foundation Trials LLC.|Bayer | August 17 2021 | Phase 2 |
| NCT04655365 | Not yet recruiting | Drug: Enzalutamide capsule | Prostate Cancer | CHU de Quebec-Universite Laval|Astellas Pharma Europe Ltd. | January 4 2021 | Phase 2 |
| NCT04456049 | Not yet recruiting | Drug: Enzalutamide | COVID-19 Infection | Ricardo Pereira Mestre|Oncology Institute of Southern Switzerland|Institute of Oncology Research|Institute for Research in Biomedicine|Ente Ospedaliero Cantonale Bellinzona | July 2020 | Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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