Enzalutamide
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- CAS-Nr.
- 915087-33-1
- Englisch Name:
- Enzalutamide
- Synonyma:
- CS-355;101095;MDV-3100;Mr Amine;Ezalutamide;EnzalutaMide;Enzalutamide API;Enzalutamide, >=99%;brand name: Xtandi.;ENZALUTAMIDE;MDV-3100
- CBNumber:
- CB62500946
- Summenformel:
- C21H16F4N4O2S
- Molgewicht:
- 464.44
- MOL-Datei:
- 915087-33-1.mol
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Enzalutamide Eigenschaften
- Schmelzpunkt:
- 198 - 200°C
- Dichte
- 1.49
- storage temp.
- -20°C
- L?slichkeit
- Soluble in DMSO (>25 mg/ml)
- Aggregatzustand
- solid
- pka
- 13.88±0.46(Predicted)
- Farbe
- White to off-white
- Stabilit?t:
- Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
- InChI
- InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)
- InChIKey
- WXCXUHSOUPDCQV-UHFFFAOYSA-N
- SMILES
- C(NC)(=O)C1=CC=C(N2C(=S)N(C3=CC=C(C#N)C(C(F)(F)F)=C3)C(=O)C2(C)C)C=C1F
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H227 |
Combustible liquid |
Flammable liquids |
Category 4 |
Warnung |
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P210, P280, P370+P378, P403+P235,P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
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| Sicherheit |
| P210 |
Von Hitze, hei?en Oberfl?chen, Funken, offenen Flammen und anderen Zündquellenarten fernhalten. Nicht rauchen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P337+P313 |
Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P370+P378 |
Bei Brand: zum L?schen verwenden. |
| P403+P235 |
An einem gut belüfteten Ort aufbewahren. Kühl halten. |
| P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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Enzalutamide Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 docetaxel. 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 (IC
50=21 nM compared with bicalutamide IC
50=160 nM), and inhibited AR translocation to the nucleus more potently than bicalutamide.The primary metabolite is the result of CYP2C8-mediated N-demethylation; enzalutamide is primarily eliminated by hepatic metabolism.
Chemische Eigenschaften
White Solid
Verwenden
MDV3100, known as Enzalutamide, is a second-generation androgen receptor (AR) signaling inhibitor. It is able to inhibit binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA.
Definition
ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant p
ostate cancer.
Clinical Use
In August 2012, the FDA approved enzalutamide, marketed by Medivation and Astellas Pharma US
for the treatment of metastatic castration-resistant prostate cancer (CRPC), specifically for those patients
who had previously received docetaxel. Enzalutamide is an inhibitor of androgen receptors (AR)—
whose increased expression has been closely linked with castration-resistant prostate cancer (CRPC),thus, AR inhibitors have seen increased recent attention from the medicinal chemistry community.
Phase I/II trials were particularly promising for enzalutamide, as 43% of patients showed >50%
sustained suppression of a key serum biomarker.
Enzalutamide Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Enzalutamide Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 523)Lieferanten
915087-33-1()Verwandte Suche:
- 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
- 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N
- BenzaMide,4-[3-[4-cyano-3-(trifluoroMethyl)phenyl]-5,5-diMethyl-4-oxo-2-thioxo-1-iMidazolidinyl]-2-fluoro-N-Methyl-
- 4-[3-(4-Ethynyl-3-trifluoromethyl-phenyl)-5,5-dimethyl-4-oxo-2-thioxo-imidazolidin-1-yl]-2-fluoro-N-methyl-benzamide
- 4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide MDV 3100
- MDV3100,Menzalutamide
- Xtandi (enzalutamide) (androgen receptor inhibitor)
- 4-Thiazolecarboxylic acid, 2-[(2,4,5-trimethoxybenzoyl)amino]-ethyl ester
- Enzalutamide, >=99%
- 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluor
- brand name: Xtandi.
- MDV-3100; MDV 3100. ENZALUTAMIDE; BRAND NAME: XTANDI.
- CS-355
- 4-{3-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-5,5-DIMETHYL-4-OXO-2-SULFANYLIDENEIMIDAZOLIDIN-1-YL}-2-FLUO
- 101095
- Enzalutamide (Xtandi)
- Ezalutamide
- 5-dimethyl-4-oxo-2-thioxoimid
azolidin-1-yl)-2-fluoro-Nmethylbenzamide
- 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5
- ENZALUTAMIDE 915087-33-1 MDV3100
- 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N(For export only)
- Enzalutamide USP/EP/BP
- 4-Isothiocyanato-2-trifluoromethylbenzonitrile, 4-Isothiocyanato-2-(trifluoromethyl)benzonitril
- 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-...
- EnzalutamideQ: What is
Enzalutamide Q: What is the CAS Number of
Enzalutamide Q: What is the storage condition of
Enzalutamide Q: What are the applications of
Enzalutamide
- Mr Amine
- Enzalutamide API
- 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide? (Enzalutamide Impurity)
- Enzalutamide, 10 mM in DMSO
- 915087-33-1
- C21H16F4N4O2S
- Apoptosis
- Aromatics
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Sulfur & Selenium Compounds
- Inhibitor
- 1
- API
- 915087-33-1
