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首页-抗体药物偶连体和PROTACs-PROTAC-PLX-4104
PLX-4104

Chemical Structure : PLX-4104

CAS No.: 2851986-77-9

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PLX-4104 (PLX4104)

货号: PC-26898Not For Human Use, Lab Use Only.

PLX-4104 is a potent, selective monovalent DCAF11-acting degrader of BRD4 with DC50 of 2 nM and Dmax of >95% in MV411 cells (24 h), shows antiproliferative activity with IC50 of 4 nM on MV-4-11 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PLX-4104 is a potent, selective monovalent DCAF11-acting degrader of BRD4 with DC50 of 2 nM and Dmax of >95% in MV411 cells (24 h), shows antiproliferative activity with IC50 of 4 nM on MV-4-11 cells.
PLX-4104 has IC50 of 4 nM in NanoBRET target engagement BET BRD assays.
PLX-4104 acts through the E3 ligase DCAF11.
PLX-4104 (2 and 6 mg/kg, PO) showed promising activity in vitro and complete tumor regression in NOD/SCID mice bearing MV-4-11 subcutaneous tumors.

物理化学性质&存储条件

分子量 619.68
分子式 C32H26FN9O2S
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

(S)-N-(4'-(6-(2-amino-2-oxoethyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-4-fluoro-[1,1'-biphenyl]-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

参考文献

1. Leriche G, et al. ACS Med Chem Lett. 2026 Apr 6;17(5):1106-1113.

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