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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
wild-type androgen receptor
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "wild-type androgen receptor" in MCE Product Catalog:
11
11 Publications Verification
Cat. No.: HY-16985
CAS No.: 1297538-32-9
Synonyms: ODM-201; BAY-1841788
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Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
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6 Cited Publications
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ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
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Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate 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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UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
Cat. No.: HY-N0475
CAS No.: 74285-86-2
Synonyms: Hypolide; (+)-Triptophenolide
Cat. No.: HY-16985S
CAS No.: 2484757-20-0
Synonyms: ODM-201-d4; BAY-1841788-d4
Cat. No.: HY-175652
CAS No.: 3056515-10-4
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AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
Cat. No.: HY-16985R
CAS No.: 1297538-32-9
Synonyms: ODM-201 (Standard); BAY-1841788 (Standard)
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Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
Cat. No.: HY-148777
CAS No.: 2682255-44-1
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A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer .
Cat. No.: HY-162764
CAS No.: 2902679-11-0
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Androgen receptor degrader-5 is an androgen receptor (AR) degrader. Androgen receptor degrader-5 induces proteasome-dependent degradation of androgen receptor protein and inhibits the transcriptional activity of wild-type AR and AR F876L. Androgen receptor degrader-5 exhibits anticancer activity against prostate cancer. Androgen receptor degrader-5 can be used in the research of prostate cancer .
Cat. No.: HY-115282
CAS No.: 2110426-27-0
Synonyms: TRC-253 free base
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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) .
Cat. No.: HY-403733A
CAS No.: 1998094-23-7
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(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
Cat. No.: HY-403733C
CAS No.: 2020353-42-6
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JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
Cat. No.: HY-183667
CAS No.: 1332390-06-3
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JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer .
Cat. No.: HY-N0475R
CAS No.: 74285-86-2
Synonyms: Hypolide (Standard); (+)-Triptophenolide (Standard)
Cat. No.: HY-151266
CAS No.: 2883447-45-6
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AR antagonist 4 is an orally active androgen receptor (AR) antagonist with a DC50 of 2.84 μM in LNCaP human prostate cancer cells. AR antagonist 4 inhibits dihydrotestosterone-induced AR transcriptional activity, promotes proteasome-dependent AR degradation, and dose-dependently promotes AR-V7 degradation. AR antagonist 4 can be used for the research of metastatic castration-resistant prostate cancer .
Cat. No.: HY-182809
CAS No.: 1372688-55-5
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Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research .
Cat. No.: HY-19337S
CAS No.: 2484757-41-5
Synonyms: BAY 1896953-d3; ORM-15341-d3
Cat. No.: HY-19337S1
Synonyms: BAY 1896953-d6; ORM-15341-d6
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
