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

CAS: 915087-33-1 Cat. No.: E407899 分子式: C₂₁H₁₆F₄N₄O₂S 分子量: 464.44 EC番号: 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

概要

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

同義語

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

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ANTAGONIST

作用メカニズム

Androgen Receptor antagonist

製品の性質

ALogP

3.6

名前と識別子

異性体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

代替CAS番号

915087-33-1

MeSH用語

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

分子量

464.44

Reaxy-Rn

11718700

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11718700&ln=

関連ターゲット（人間）

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)