Proxalutamide( GT-0918 | GT 0918 )

Catalog No. M11663 CAS No. 1398046-21-3

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Product Name

Proxalutamide
Note

Research use only, not for human use.
Brief Description

A potent androgen receptor (AR) antagonist with ability to down regulate AR protein level in prostate cancer cells.
Description

A potent androgen receptor (AR) antagonist with ability to down regulate AR protein level in prostate cancer cells; more potently inhibits androgen binding with AR's ligand binding domain than Bicalutamide (11.4-fold) and MDV3100 (3.5-fold) in biochemical assay; demonstrates stronger potency to block AR function of gene transcription in CRPC cells; demonstrates good anti-tumor efficacy among hormone sensitive, CRPC and AR+ breast cancer animal models.Prostate Cancer Phase 2 Clinical.
In Vitro

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In Vivo

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Synonyms

GT-0918 | GT 0918
Pathway

Endocrinology/Hormones
Target

Androgen Receptor (AR)
Recptor

Androgen Receptor (AR)
Research Area

Cancer
Indication

Prostate Cancer

CAS Number

1398046-21-3
Formula Weight

517.5
Molecular Formula

C24H19F4N5O2S
Purity

>98% (HPLC)
Solubility

——
SMILES

N#CC1=CC=C(N(C(N(C2=CC=C(CCCC3=NC=CO3)N=C2)C4(C)C)=S)C4=O)C(F)=C1C(F)(F)F
Chemical Name

4-[4,4-Dimethyl-3-[6-[3-(2-oxazolyl)propyl]-3-pyridinyl]-5-oxo-2-thioxo-1-imidazolidinyl]-3-fluoro-2-(trifluoromethyl)benzonitrile

1. Youzhi Tong, et al. DOI: 10.1158/1538-7445.AM2014-614 Published October 2014 2. Yang M, et al. Int J Pharm. 2014 Nov 20;475(1-2):97-109.

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