enzalutamide

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

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 potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide.

Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.

Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide. Enzalutamide carboxylic acid D6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid).

Enzalutamide-d6 Carboxylic Acid is a deuterated compound of Enzalutamide Carboxylic Acid. Enzalutamide Carboxylic Acid has a CAS number of 1242137-15-0. Enzalutamide carboxylic acid is an antagonist of androgen receptor (AR) .

N-desmethyl Enzalutamide D6 is a deuterium labeled N-desmethyl Enzalutamide.

Enzalutamide carboxylic acid is an antagonist of androgen receptor (AR) .

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 synergistically with the AR antagonist enzalutamide.AU-15330 shows partial therapeutic efficacy and non-toxicity with the AR antagonist enzalutamide in a desmoplasia-resistant prostate cancer (CRPC) model. AU-15330 showed partial therapeutic efficacy in a denervation-resistant prostate cancer (CRPC) model and AU-15330 was characterized by non-toxicity.

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 inhibits Prostate Specific Antigen (PSA) in both LNCaP and MR49F and reduces expression of AR target genes, PSA and TMPRSS2. These findings suggest that VPC-13566 exhibits AR BF3 specific mechanism of action.

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 desmoplasia-resistant prostate cancer.

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-prostate cancer efficacy.

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 under investigation for potential use in research on enzalutamide-resistant prostate cancer [1].

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 exhibits antitumor activity against enzalutamide resistant debulking resistant prostate cancer (CRPC).

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 degrades clinically relevant AR mutants associated with antiandrogen therapy[1].