LYA914

Chemical Structure : LYA914

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货号: 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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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	747.86
分子式	C38H43F2N7O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Yan Lv, et al. J Med Chem. 2025 Jul 28. doi: 10.1021/acs.jmedchem.5c01463.

LYA914

生物&药学活性

物理化学性质&存储条件

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LYA914

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