Chemical Structure : LYA914
CAS No.:
LYA914
Catalog No.: PC-25306Not For Human Use, Lab Use Only.
LYA914 is a potent, specific PROTAC degrader targeting the conserved DNA binding domain (DBD) of androgen receptor (AR) with DC50 of 0.45 uM and 0.34 uM for AR and AR-V7 in 22Rv1 cells, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LYA914 is a potent, specific PROTAC degrader targeting the conserved DNA binding domain (DBD) of androgen receptor (AR) with DC50 of 0.45 uM and 0.34 uM for AR and AR-V7 in 22Rv1 cells, respectively.
LYA914 effectively inhibits the transcription activity of AR and AR-V7.
LYA914 inhibits cell growth with IC50 of 1.21 μM for LNCaP, an AR-positive and androgen-dependent cell line.
LYA914 exhibits antiproliferative effects against LNCaP-EN and VCaP-EN cells, with IC50 values of 4.12 and 1.66 μM, respectively, which is more than 10-fold potent compared with enzalutamide.
LYA914 effectively inhibits proliferation of enzalutamide-resistant cells and the transcription activity of AR mutants (F876L, W741L).
LYA914 (100 mpk, i.p.) exhibits in vivo degradation and antitumor efficiency in LNCaP xenograft model in NOD-SCID mice.
Physicochemical Properties
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M.Wt
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747.86
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Formula
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C38H43F2N7O5S
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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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5-(4-((4-(4-(4-(3,4-Difluoro-2-methoxyphenyl)thiazol-2-yl)piperazin-1-yl)piperidin-1-yl)methyl)piperidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
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References
1. Yan Lv, et al. J Med Chem. 2025 Jul 28. doi: 10.1021/acs.jmedchem.5c01463.
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