Chemical Structure : AR inhibitor 1ae
CAS No.:
2920732-75-6
AR inhibitor 1ae
(Compound 1ae)
Catalog No.: PC-21502Not For Human Use, Lab Use Only.
AR inhibitor 1ae is a small-molecule inhibitor of the androgen receptor activation domain (AR AD) with IC50 of 1.54 uM in androgen-induced PSA-luciferase assays, inhibits AR-V7 transcriptional activity with IC50 of 4.1 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AR inhibitor 1ae is a small-molecule inhibitor of the androgen receptor activation domain (AR AD) with IC50 of 1.54 uM in androgen-induced PSA-luciferase assays, inhibits AR-V7 transcriptional activity with IC50 of 4.1 uM.
1ae inhibits AR-dependent targets in prostate cancer cells and is more potent in its transcriptional inhibitory effect than EPI-001 (Cat#PC-61678).
1ae significantly reduced tumor volumes in both the LNCaP and LNCaP95-D3 xenograft models.
1ae outperformed enzalutamide in the AR-V7-driven LNCaP95-D3 xenograft model of CRPC.
Physicochemical Properties
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M.Wt
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452.93
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Formula
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C26H25ClO5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-3-(4-((6-((S)-3-chloro-2-hydroxypropoxy)-[1,1'-biphenyl]-3-yl)ethynyl)phenoxy)propane-1,2-diol
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References
1. Basu S, et al. Nat Struct Mol Biol. 2023 Dec 4. doi: 10.1038/s41594-023-01159-5.
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