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Search Results for " enzalutamide "

14

Compounds

Cat No. Product Name Synonyms Targets
T6002 Enzalutamide MDV3100 Androgen Receptor , Autophagy
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate canc...
T8217 Enzalutamide carboxylic acid Androgen Receptor , Drug Metabolite
Enzalutamide carboxylic acid is an antagonist of androgen receptor (AR) .
T19450 N-desmethyl Enzalutamide N-desmethyl MDV 3100 Androgen Receptor
N-desmethyl Enzalutamide (N-desmethyl MDV 3100) is the active Enzalutamide metabolite.It is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar p...
T11208 Enzalutamide-d3 MDV3100 D3 Others
Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
T19449 N-desmethyl Enzalutamide D6 N-desmethyl MDV 3100 D6 Androgen Receptor
N-desmethyl Enzalutamide D6 is a deuterium labeled N-desmethyl Enzalutamide.
T19311 Enzalutamide carboxylic acid D6 MDV3100 carboxylic acid D6 Others
Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide. Enzalutamide carboxylic acid D6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid).
T13273 UT-34 Androgen Receptor
UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prost...
T69564 YK-2-69
YK-2-69 is a highly selective DYRK2 inhibitor which specifically interacts with Lys-231 and Lys-234 in the co-crystal structure. Especially, YK-2-69 exhibits more potent anti-PCa efficacy than the first-line drug enzalut...
T29214 ZEN-3694 ZEN 3694,ZEN3694 Epigenetic Reader Domain
ZEN-3694 (ZEN 3694) is a bromo-structural domain extra-terminal inhibitor (BETi) with activity in androgen signaling inhibitor (ASI) resistance models and can be used in combination with enzalutamide to study metastatic ...
T29110 VPC-13163 2,3-dihydro-2,3'-Bi-1H-indole,VPC13163,NSC52361,NSC 52361,VPC 13163 Others
VPC-13163 (NSC-52361) has strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhib...
T39954 AU-15330 Epigenetic Reader Domain , PROTACs
AU-15330 is a protein hydrolysis-targeted chimeric (PROTAC) degrader of the SWI/SNF ATPase subunits SMARCA2 and SMARCA4.AU-15330 potently inhibits tumor growth in a prostate cancer xenograft model and acts synergisticall...
T14318 ARCC-4 Others
ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively...
T63811 EPI-7170
EPI-7170 is a ralaniten analogue and a potent antagonist of the androgen receptor N-terminal structural domain, blocking the transcriptional activity of the full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170...
T79519 YXG-158 Androgen Receptor
YXG-158 (Compound 23-h), an orally active androgen receptor (AR) degrader and cytochrome P450 17A1 (CYP17A1) inhibitor, exhibits AR degradation with a DC50 of 1.28 μM and CYP17A1 inhibition with an IC50 of 100 nM. It is ...
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