HPK1 PROTAC C3

Chemical Structure : HPK1 PROTAC C3

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货号: PC-22897Not For Human Use, Lab Use Only.

HPK1 PROTAC C3 is a potent, selective and orally active HPK1 PROTAC degrader with DC50 of 21.26 nM, Dmax of 80.50% in Jurkat cells.

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生物&药学活性

HPK1 PROTAC C3 is a potent, selective and orally active HPK1 PROTAC degrader with DC50 of 21.26 nM, Dmax of 80.50% in Jurkat cells.
HPK1 PROTAC C3 does not significantly impact other family proteins like GCK and HGK.
HPK1 PROTAC C3 showed degradation selectivity and potent immune activation effects.
Oral administration of C3 in combination with anti-PDL1 antibody significantly inhibited tumor growth (tumor growth inhibition = 65.58%).

物理化学性质&存储条件

分子量	750.86
分子式	C43H42N8O5
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(2-(4-(1-(1-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)piperidin-4-yl)phenyl)-5H-pyrrolo[2,3-b]pyrazin-7-yl)-N,N,2-trimethylbenzamide

参考文献

1. Mingfei Wu, et al. J Med Chem. 2024 Jul 31. doi: 10.1021/acs.jmedchem.4c00644.

HPK1 PROTAC C3

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物理化学性质&存储条件

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HPK1 PROTAC C3

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