Enzalutamide (MDV3100) - Moligand™, 10mM in DMSO , Androgen Receptor antagonist, CAS No.915087-33-1, Androgen Receptor antagonist

CAS: 915087-33-1 Cat. No.: E407899 Peso molecular: 464.44 Número EC: 805-022-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5,​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy .
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). Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.

In vivo

Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：1-4 days

Powder Purity:≥99%

Specifications

Sinónimos

4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5, ​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ANTAGONIST

Mecanismo de acción

Androgen Receptor antagonist

Propiedades del producto

• ALogP: 3.6

Nombres e identificadores

• Isómeros 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
• CAS alternativo: 915087-33-1
• Términos de entrada MeSH: 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-(methyl-d3)benzamide;4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-methyl-benzamide;enzalutamide;enzaluta
• Peso molecular: 464.44
• Reaxy-Rn: 11718700
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11718700&ln=

Objetivos asociados (humanos)

KLK3 Tclin Prostate-specific antigen (1 Activities)

Discover Target: KLK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor (12 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Referencias

1. Jiang Zhihui, Zhou Bo, Li Xinping, Kirby Gordon M., Zhang Xiaoying.  (2018)  Echinacoside Increases Sperm Quantity in Rats by Targeting the Hypothalamic Androgen Receptor.  Scientific Reports,  8  (1): (1-11).  [PMID:29497114] [10.1038/s41598-018-22211-1]

2. Shijia Lu, Chenxiao Zhang, Huiru Wu, Junjie Wang, Jinglong Wang, Limei Zhao, Tianyang Ren, Guofei Li.  (2025)  A pH/MMP-9 smart dual-responsive liposome GBE@LP co-delivers and controls the release of GB1107/BMS1166/Enzalutamide for liver cancer immunotherapy.  Materials Today Bio,      [PMID:40475856] [10.1016/j.mtbio.2025.101801]

3. Tingting Zheng, Hang Yin, Hongna Shan, Lihuan Sun, Lili Jiang, Yong Liu.  (2025)  Synergistic inhibitory effects of enzalutamide and its phase I metabolite on UDP-glucuronosyltransferase 1A1 (UGT1A1) and risk prediction of drug-drug interactions.  CHEMICO-BIOLOGICAL INTERACTIONS,      [PMID:41241169] [10.1016/j.cbi.2025.111829]