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首页-抗体药物偶连体和PROTACs-PROTAC-ATC-324
ATC-324

Chemical Structure : ATC-324

CAS No.: 2925060-81-5

ATC-324 (ACT324)

货号: PC-23448Not For Human Use, Lab Use Only.

ATC-324 is a potent, selective androgen receptor (AR) AUTOphagy-TArgeting Chimera (AUTOTAC) degrader with DC50 of 2.05 uM in LNCaP cells, induces the formation of the AR/p62 complex, leading to autophagy-lysosomal degradation of AR.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ATC-324 is a potent, selective androgen receptor (AR) AUTOphagy-TArgeting Chimera (AUTOTAC) degrader with DC50 of 2.05 uM in LNCaP cells, induces the formation of the AR/p62 complex, leading to autophagy-lysosomal degradation of AR.
ATC-324 demonstrates sustained and progressive degradation of AR proteins over 24 hours, through p62-mediated autophagy.
ATC-324 induces cytotoxicity involving apoptosis in AR-positive prostate cancer cells.
ATC-324 degrades not only full-length AR proteins but also the AR splice variant AR-v7.
ATC-324 at a dose of 20 mg/kg through intraperitoneal (i.p.) injection effectively suppressed tumor growth in both 22Rv1 and LNCaP models, remains potent in enzalutamide-resistant PCa cells.

物理化学性质&存储条件

分子量 1068.10
分子式 C53H55F6N5O10S
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

(R)-N-(18-(3,4-bis((4-fluorobenzyl)oxy)phenoxy)-17-hydroxy-3,6,9,12-tetraoxa-15-azaoctadecyl)-4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluorobenzamide

参考文献

1. Bae TH, et al. Cancer Res. 2024 Nov 12. doi: 10.1158/0008-5472.CAN-24-0591.

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