Customization: | Available |
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CAS No.: | 915087-33-1 |
Formula: | C21h16f4n4o2s |
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Product Name: Enzalutamide
Synonyms: 4-{3-[4-cyano-3-(trifluoroMethyl)phenyl]-5,5-diMethyl-4-oxo-2-sulfanylideneiMidazolidin-1-yl}-2-fluoro-N-MethylbenzaMide;EnzalutaMide;MDV3100 (EnzalutaMide);ENZALUTAMIDE;MDV-3100;MDV-3100;4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide;4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide;MDV 3100,4-[3-[4-Cyano-3-(trifluoroMethyl)phenyl]-5,5-diMethyl-4-oxo-2-thioxo-1-iMidazolidinyl]-2-fluoro-N-MethylbenzaMide
CAS: 915087-33-1
MF: C21H16F4N4O2S
MW: 464.44
EINECS: 805-022-1
Description:
In August 2012, the US FDA approved enzalutamide for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously been treated with doce taxel. Synthesis of enzalutamide was achieved by a triply convergent route that employed a Strecker condensation, followed by isothiocyanate condensation and hydrolysis to form the thiohydantoin moiety. In LNCaP/AR cells with high expression of AR, enzalutamide demonstrated potent inhibition of 16b-[18F]-5α-dihydrotestosterone binding (IC50=21 nM compared with bicalu tamide IC50=160 nM), and inhibited AR translocation to the nucleus more potently than bicalu tamide.The primary metabolite is the result of CYP2C8-mediated N-demethylation; enzalutamide is primarily eliminated by hepatic metabolism.
Usage:
MDV 3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. MDV 3100 has also been shown to induce tumor cell apoptosis, and has no agonist activity. MDV 3100 is a candidate for the treatment of castration-resistant prostate cancer.
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Hubei Yuanmeng Biological Technology Co., Ltd.
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Fiona Wei