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Chemical Structure : AR inhibitor 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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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.
| M.Wt | 452.93 | |
| Formula | C26H25ClO5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Basu S, et al. Nat Struct Mol Biol. 2023 Dec 4. doi: 10.1038/s41594-023-01159-5.
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