Androgen receptor degrader-5
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 ARF876L. Androgen receptor degrader-5 exhibits anticancer activity against prostate cancer. Androgen receptor degrader-5 can be used in the research of prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 2902679-11-0
- Formula: C29H25F4N5O2
- Molecular Weight:551.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
Description
In Vitro
Androgen receptor degrader-5 (Compound 14k) (7 days) potently inhibits proliferation of 22Rv1 Enzalutamide (HY-70002)-resistant prostate cancer cells with an IC50 of 0.838 μM[1].
Androgen receptor degrader-5 (7 days) inhibits proliferation of LNCaP wild-type prostate cancer cells with an IC50 of 1.75 μM[1].
Androgen receptor degrader-5 (7 days) potently inhibits proliferation of LNCaP-Enz-R enzalutamide-resistant prostate cancer cells with an IC50 of 4.68 μM[1].
Androgen receptor degrader-5 (1-10 μM; 24 h) degrades AR protein in 22Rv1 prostate cancer cells, with 10 μM treatment reducing AR levels to 0.36 relative to β-actin after 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 prostate cancer cells
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Concentration:1-10 μM
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Incubation Time:24 h
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Result:Reduced AR protein levels to 0.80 relative to β-actin at 1 μM.
Reduced AR protein levels to 0.36 relative to β-actin at 10 μM.
Chemical Information
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CAS No. 2902679-11-0
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Molecular Weight 551.53
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Formula C29H25F4N5O2
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SMILES
O=C([C@@](C)(O)CN1CCN(C2=CC=C(C3=CC(F)=C(C#N)C=C3)C=C2)CC1)NC4=CC=C(C#N)C(C(F)(F)F)=C4
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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 degrader-5 Related Classifications
HY-162764 Related Classifications
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Keywords
- Androgen receptor degrader-5
- 2902679-11-0
- Androgen receptor degrader5
- Androgen receptor degrader 5
- Androgen Receptor
- human mutant androgen receptor (AR-F876L)
- androgen receptor
- prostate cancer cells
- human wild-type androgen receptor
- ICR mice
- HEK293 cells
- 22Rv1 enzalutamide-resistant prostate cancer cells
- LNCaP wild-type prostate cancer cells
- enzalutamide-resistant prostate cancer
- proteasome-dependent degradation
- Inhibitor
- inhibitor
- inhibit