Search Result
Results for "
castration-resistant prostate cancer (CRPC)
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-111503
-
|
Epigenetic Reader Domain
|
Cancer
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Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
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- HY-10088
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ZD4054
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cancer
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Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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- HY-124628
-
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Fatty Acid Synthase (FASN)
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Cancer
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IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
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- HY-P99217
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AMG 102
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c-Met/HGFR
|
Cancer
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Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
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- HY-109070
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EPI-002
|
Androgen Receptor
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Cancer
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Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-145388
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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- HY-149894
-
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Biochemical Assay Reagents
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Cancer
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MC-1-F2 is a FOXC2 inhibitor that reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC .
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-
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- HY-164552
-
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Apoptosis
Androgen Receptor
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Cancer
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ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
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- HY-137193
-
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Drug Metabolite
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Cancer
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5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer) .
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- HY-139970
-
|
Androgen Receptor
|
Endocrinology
Cancer
|
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
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- HY-70006
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TOK-001; VN-124-1
|
Cytochrome P450
|
Cancer
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Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
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- HY-115282A
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TRC-253
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Androgen Receptor
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Cancer
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JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-10088R
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ZD4054 (Standard)
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Reference Standards
Endothelin Receptor
Apoptosis
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Endocrinology
Cancer
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Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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- HY-150102
-
|
Androgen Receptor
|
Cancer
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EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
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- HY-115282
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TRC-253 free base
|
Androgen Receptor
|
Cancer
|
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
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- HY-111061
-
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Estrogen Receptor/ERR
|
Cancer
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GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research .
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- HY-10617D
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AG014699 acetate; PF-01367338 acetate
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PARP
|
Cancer
|
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617
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AG-014699 phosphate; PF-01367338 phosphate
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PARP
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Cancer
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Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617A
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Rucaparib
Maximum Cited Publications
42 Publications Verification
AG014699; PF-01367338
|
PARP
|
Cancer
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Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
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-
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- HY-10617B
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AG014699 hydrochloride; PF-01367338 hydrochloride
|
PARP
|
Cancer
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Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617C
-
AG-014699 tartrate; PF-01367338 tartrate
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PARP
|
Cancer
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Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-161700
-
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Cytochrome P450
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Cancer
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BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels .
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- HY-102003A
-
AG014699 camsylate; PF-01367338 camsylate
|
PARP
|
Cancer
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Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-102003
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AG014699 monocamsylate; PF-01367338 monocamsylate
|
PARP
|
Cancer
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Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617AR
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AG014699 (Standard); PF-01367338 (Standard)
|
Reference Standards
PARP
|
Cancer
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Rucaparib (Standard) is the analytical standard of Rucaparib. This product is intended for research and analytical applications. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-10617R
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AG-014699 phosphate (Standard); PF-01367338 phosphate (Standard)
|
PARP
|
Cancer
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Rucaparib (phosphate) (Standard) is the analytical standard of Rucaparib (phosphate). This product is intended for research and analytical applications. Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-42424
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VHL ligand 2 hydrochloride; E3 ligase Ligand 1
|
Ligands for E3 Ligase
|
Cancer
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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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- HY-42424A
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VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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- HY-10617AS
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AG014699-d8 ; PF-01367338-d8
|
Isotope-Labeled Compounds
PARP
|
Cancer
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Rucaparib-d8 (AG014699-d8 ) is deuterium labeled Rucaparib. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
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- HY-112078
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VHL ligand 2; E3 ligase Ligand 1A
|
Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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- HY-N0790
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Lupeol
3 Publications Verification
Clerodol; Monogynol B; Fagarasterol
|
Androgen Receptor
Apoptosis
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Cancer
|
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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-
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- HY-138557
-
|
17β-HSD
|
Cancer
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AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .
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- HY-N0790R
-
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Androgen Receptor
Apoptosis
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Cancer
|
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
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- HY-163410
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
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- HY-170820
-
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Molecular Glues
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Cancer
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XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
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-
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- HY-155666
-
|
Androgen Receptor
|
Cancer
|
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .
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-
-
- HY-160777
-
Galeterone 3β-imidazole
|
Molecular Glues
Androgen Receptor
MNK
Apoptosis
|
Cancer
|
VNPP433-3β (Galeterone 3β-imidazole) is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2.VNPP433-3β induces cell apoptosis. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99217
-
AMG 102
|
c-Met/HGFR
|
Cancer
|
Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10617AS
-
|
Rucaparib-d8 (AG014699-d8 ) is deuterium labeled Rucaparib. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
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