Enzalutamide (MDV3100)

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

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Enzalutamide MDV3100 915087-33-1

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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.

Targets

Androgen Receptor [1]
(LNCaP cells)

36 nM

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
human LNCAP	Cytotoxic Assay		7 days	95% EtOH	IC50=5.12 μM	23713567
human LNCAP	Function Assay	1 μM		DMSO	Inhibits prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 100-1000nM	20218717
VCaP	Function Assay	10 μM	24 h	DMSO	Suppresses ligand-mediated AR-FL signaling	22710436

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7; AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166); CXCR7;	28607007 26378044 29277895
Growth inhibition assay	Cell proliferation;	28115200
Immunofluorescence	AR; pAKT(S473); CXCR7;	27588408 29277895
ELISA	osteoprotegerin;	27015557

In vivo

Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]

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