Androgen receptor antagonist-14
Androgen receptor antagonist-14 (Compound S-94) is a selective antagonist of the T878A mutant androgen receptor (AR) with an IC50 of 0.38 μM. Androgen receptor antagonist-14 selectively antagonizes the transcriptional activity of the ART878A, ARF877L/T878A and ARH875Y/T878A mutant androgen receptors. Androgen receptor antagonist-14 exhibits anticancer activity against prostate cancer. Androgen receptor antagonist-14 can be used in the research of prostate cancer.
For research use only. We do not sell to patients.
- Formula: C26H25N3O3
- Molecular Weight:427.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ART878A 0.38 μM (IC50) |
Androgen receptor antagonist-14 potently inhibits the transcriptional activity of T878A-mutated AR in LNCaP-ARR2PB-eGFP cells, with an IC50 of 0.38 μM[1].
Androgen receptor antagonist-14 (0.1-10 μM; 48 h) dose-dependently reduces the expression of DHT-induced AR target genes PSA, UBE2C and KLK2 in LNCaP cells without altering AR mRNA levels[1].
Androgen receptor antagonist-14 (0.1-10 μM; 48 h) dose-dependently reduces PSA protein levels in LNCaP cells without altering AR protein levels[1].
Androgen receptor antagonist-14 (3 days) selectively inhibits the proliferation of LNCaP cells with an IC50 of 10.32 μM, while it exhibits only extremely low cytotoxicity against other prostate cancer cell lines and non-cancerous cell lines[1].
Androgen receptor antagonist-14 (10 μM; 24 h) induces G1-phase cell cycle arrest in LNCaP cells and reduces the mRNA expression of key cell cycle regulators Cyclin A, CDC20 and CDK1[1].
Androgen receptor antagonist-14 (4 h) exhibits weak binding affinity for the ligand-binding pocket of wild-type AR, with an IC50 value of 85.60 μM[1].
Androgen receptor antagonist-14 potently and selectively inhibits the transcriptional activity of DHT-induced T878A mutant AR in HEK293T cells (IC50 = 0.49 μM), while its activity against wild-type AR is over 50-fold lower (IC50 = 27.18 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP (harboring endogenous T878A-mutant AR)
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Concentration:0.1-10 μM
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Incubation Time:48 h
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Result:Reduced DHT-induced transcriptional activation of the AR downstream target genes PSA, UBE2C, and KLK2 in a dose-dependent fashion.
Did not affect mRNA expression of AR itself.
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Cell Line:LNCaP (harboring endogenous T878A-mutant AR)
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Concentration:0.1-10 μM
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Incubation Time:48 h
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Result:Decreased endogenous PSA protein levels in a dose-dependent manner.
Caused no significant alteration in AR protein levels.
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Cell Line:LNCaP, C4-2B, PC3, WPMY-1, NIH-3T3, DU145, GES-1, Chang, 22RV1
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Concentration:Gradient concentrations
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Incubation Time:3 days
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Result:Inhibited proliferation of LNCaP cells with an IC50 of 10.32 μM.
Exhibited minimal inhibitory effects on C4-2B, 22RV1, DU145, and PC3 prostate cancer cell lines.
Showed minimal cytotoxicity in non-cancerous WPMY-1, GES-1, Chang, and NIH-3T3 cell lines.
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Cell Line:LNCaP (harboring endogenous T878A-mutant AR)
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Concentration:10 μM (cell cycle assay); 0.1-10 μM (qPCR)
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Incubation Time:24 h (cell cycle assay); 48 h (qPCR)
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Result:Decreased the S phase population and increased the G1 phase population in LNCaP cells compared to DMSO control.
Significantly reduced mRNA levels of the cell cycle regulators Cyclin A, CDC20, and CDK1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 3-4 weeks old, subcutaneous flank injection of LNCaP-FGC cells harboring T878A-mutant AR)[1]
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Dosage:40 mg/kg; 20 mg/kg
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Administration:i.g.; daily; 26 days; i.p.; daily; 26 days
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Result:Suppressed LNCaP tumor growth relative to vehicle control.
Significantly reduced tumor weight compared to vehicle at 20 mg/kg i.p. dose.
Decreased Ki67-positive staining (lower tumor cell proliferation) at 20 mg/kg i.p. dose.
Significantly decreased PSA protein levels in tumor tissues at 20 mg/kg i.p. dose.
Caused no significant weight loss or signs of toxicity throughout the study.
Chemical Information
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Molecular Weight 427.50
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Formula C26H25N3O3
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SMILES
CC1=CC(NC([C@H](CC2=CNC3=C2C=CC=C3)NC(OC4=CC=CC=C4)=O)=O)=CC(C)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Androgen receptor antagonist-14 Related Classifications
HY-183287 Related Classifications
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