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

N-desmethyl Enzalutamide-D6 is a deuterium labeled N-desmethyl Enzalutamide (T19450).

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.

Luxdegalutamide (ARV-766) is a PROTAC and a protein degrader targeting the androgen receptor, capable of effectively degrading wild-type and drug-resistant mutants including L702H, H875Y, and T878A. With oral bioactivity and cell permeability, this compound is used in castration-resistant prostate cancer research and exhibits significant antitumor activity.

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

Topterone (Win 17,665) is a potent topical antiandrogen that inhibits the stimulation of lumbar organ development by testosterone and dihydrotestosterone in castrated immature male hamsters.

Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist used in breast and prostate cancer research.

MK-0773 (PF-05314882) is a selective androgen receptor modulator that binds to AR (IC50: 6.6 nM) for the study of diseases caused by endocrine abnormalities.

MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is a selective androgen receptor modulator with an IC50 value of 6.6 nM for AR, which can be used for the prevention and treatment of cancer-related muscle wasting.

ONC1-13B is a potent androgen receptor (AR) antagonist with an ic50 in the range of 59-80 nM that inhibits PSA production in androgen-sensitive human PCa LNCaP cells.

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

VPC-13566 is a BF3-specific small molecule, which effectively inhibited the androgen receptor transcriptional activity and displaced the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines and reduces the growth of AR-dependent prostate cancer xenograft tumors in mice.

AS-601811 is a steroidal 5α-reductase inhibitor and androgen receptor modulator used to study hair loss and acne.

MK-3984 is a selective androgen receptor modulator, used in the study of conditions caused by androgen deficiency.

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.

BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer.

Zanoterone is an AR antagonist (androgen receptor).Zanoterone has antitumor activity for the treatment of genitourinary disorders and oncological disorders and may be used in the study of prostate cancer.

BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer.

Androgen receptor-IN-4 is an androgen receptor modulator.

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.

Rosolutamide (ALZ-003) is a curcumin analog, an orally active Nrf1 and Nrf2 activator.Rosolutamide modulates oxidative homeostasis, improves mitochondrial function and promotes autophagy, reduces mutant protein aggregation, and decreases intracellular/mitochondrial reactive oxygen species (ROS) levels.Rosolutamide has been used in the study of neurodegeneration such as spinal cerebellar ataxia and Huntington disease. neurodegenerative diseases such as Huntington's disease. Regulates oxidative homeostasis.

Octinoxate (Octyl 4-methoxycinnamate) is used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage,primarily as an ingredient in some sunscreens and lip balms. It is also used to reduce the appearance of scars.

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.