[CAS NO. 915087-33-1] Enzalutamide (MDV3100)

Name: Enzalutamide (MDV3100)
Brand: Arctom Scientific
SKU: SLK-S1250

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PRODUCTS SPECIFICATIONS [915087-33-1]

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Catalog

SLK-S1250

Brand

Selleck

CAS

915087-33-1

DESCRIPTION [915087-33-1]

Overview

MDL	MFCD14155804
Molecular Weight	464.44
Molecular Formula	C21H16F4N4O2S
SMILES	S=C1N(C(C)(C)C(=O)N1C2=CC(C(F)(F)F)=C(C#N)C=C2)C3=CC(F)=C(C(NC)=O)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1531 mL	10.7657 mL	21.5313 mL
5 mM	0.4306 mL	2.1531 mL	4.3063 mL
10 mM	0.2153 mL	1.0766 mL	2.1531 mL
50 mM	0.0431 mL	0.2153 mL	0.4306 mL

Description

Enzalutamide (MDV3100) is an antagonist with of 36 nM in LNCaP cells. Enzalutamide is shown to increase .

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-[F]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 Trp 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.

References

[1] Tran C, et al, Science, 2009, 324 (5928), 787-790.
[2] Scher HI, et al, Lancet, 2010, 375(9724), 1437-1446.
[3] US2007254933 A1)

Synonyms

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

4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide

MDV 3100

Enzalutamide

Xtandi

S-Enzalutamide