XZ739

Chemical Structure : XZ739

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货号: PC-24379Not For Human Use, Lab Use Only.

XZ739 is a potent, CRBN-dependent PROTAC BCL-XL degrader with DC50 of 2.5 nM (MOLT-4 cells), reduces MOLT-4 cell viability with IC50 of 10.1 nM.

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生物&药学活性

XZ739 is a potent, CRBN-dependent PROTAC BCL-XL degrader with DC50 of 2.5 nM (MOLT-4 cells), reduces MOLT-4 cell viability with IC50 of 10.1 nM.
XZ739 dose-dependently induced BCL-XL degradation in MOLT-4 cells, which can be abrogated by proteasome inhibitor MG-132.
XZ739 shows improved selectivity because of its low activity in inducing BCL-XL degradation in human platelets, and the remaining cytotoxicity to human platelets mainly depends on BCL-XL inhibition.
XZ739 does not affect IKZF1 and IKZF3 protein levels, has >100-fold selectivity for MOLT-4 cells over human platelets.

物理化学性质&存储条件

分子量	1349.99
分子式	C65H76ClF3N8O12S3
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	4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-(((15R)-1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-12-methyl-16-(phenylthio)-3,6,9-trioxa-12-azahexadecan-15-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

参考文献

1. Zhang X, et al. Eur J Med Chem. 2020 Apr 15;192:112186.

XZ739

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XZ739

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