CH5137291
CH5137291 is an orally active pure antagonist of the androgen receptor (AR), without generating agonist metabolites. CCH5137291 directly blocks the transfer of AR from the cytoplasm to the nucleus. H5137291 can completely inhibit tumor growth in cells and mouse models of castration-resistant prostate cancer models. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC).
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- CAS. Nr.: 1043446-39-4
- Formel: C18H14F3N5O3S2
- Molecular Weight:469.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
700 nM
Compound: 17b
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Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
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[PMID: 21050768] |
| LNCaP | IC50 |
100 nM
Compound: 17b
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Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
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[PMID: 21050768] |
Chemical Information
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CAS. Nr. 1043446-39-4
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Molecular Weight 469.46
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Formel C18H14F3N5O3S2
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SMILES
N#CC1=CC=C(N2C(C(C)(C)N(C2=S)C3=CC=CC(S(=O)(N)=O)=N3)=O)C=C1C(F)(F)F
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Yoshino H, et al. Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer. Bioorg Med Chem. 2010 Dec 1;18(23):8150-7. [Content Brief]
[2]. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC) [1][2]. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CH5137291 Related Classifications
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