castration-resistant

Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.

IPI-9119 is an orally active, selective, and irreversible FASN inhibitor (IC50 = 0.3 nM).

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

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

MC-1-F2 is a direct FOXC2 inhibitor with anticancer activity, inhibits cancer stem cell (CSC) characteristics, and reduces the invasive ability of castration-resistant prostate cancer (CRPC) cell lines. MC-1-F2 can be used to study prostate cancer.

Cabazitaxel (taxoid XRP6258) is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.

GDC-2992 is a selective and orally active androgen receptor (AR) degradator that degrades AR (DC50 = 2.7 nM) and inhibits proliferation (IC50 = 9.7 nM) in VCaP cells, making it suitable for studying castration-resistant prostate cancer (CRPC).

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

EC1169 is a targeted tubulysin conjugate that utilizes EC1167 as its linker. This compound shows promise in the treatment of recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1].

Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.

(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).

XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1, with a DC50 of 19 nM, used for researching MYC-driven castration-resistant prostate cancer (CRPC). It effectively inhibits the growth of 22Rv1 cells (IC50 = 7 nM) and exhibits antitumor efficacy in vivo. XYD049 downregulates CRPC-associated oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 comprises a molecular glue linker (black part) NH2-C5-NH-Boc, a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a target protein ligand (red part) GSPT1 ligand-1, with the E3 ligase ligand + linker forming the conjugate E3 Ligase Ligand-linker Conjugate 158.

PSMA-trillium is a PSMA-targeting compound comprising a PSMA-targeting molecule (PSMA binding agent), a Macropa chelator, and a pharmacokinetics-modulating group (PK modulator). It acts as the non-radioactive variant of Actinium-225-PSMA-Trillium (BAY 3563254), boasting enhanced PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind with Ac through either the Macropa chelator or the radioactive isotope Actinium-225. Actinium-225-PSMA-Trillium effectively inhibits metastatic castration-resistant prostate cancer (mCRPC).

Bavdegalutamide (ARV-110) is an oral protein degrader that specifically binds to AR and mediates its degradation. Bavdegalutamide can degrade clinically relevant mutant AR proteins, maintain activity in a high androgen environment, and has an acceptable safety profile.

BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

Histone H3K27Me1 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. Monomethylation of histone H3 at lysine 27 is associated with actively transcribed genes and positively correlates with H3K36 trimethylation. Levels of H3K27Me1 are increased in tumor tissue isolated from patients with metastatic hormone-na ve and castration-resistant prostate cancer. Histone H3K27Me1 (23-34) has been used in epitope mapping of the lupus-derived monoclonal antibody BT164.

Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.

Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.

HG122 is a chemical compound that effectively facilitates the degradation of androgen receptor (AR) via the proteasome pathway, leading to the inhibition of castration-resistant prostate cancer.

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

VPC-13789 is a highly potent, selective, and orally bioavailable antiandrogen compound that shows promise for studying and developing therapeutics for castration-resistant prostate cancer (CRPC). In LNCaP cells, VPC-13789 effectively inhibits the transcriptional activity of the androgen receptor (AR) with an IC50 value of 0.19 μM [1].