HPK1 PROTAC C3

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Chemical Structure : HPK1 PROTAC C3

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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%).

Physicochemical Properties

M.Wt	750.86
Formula	C43H42N8O5
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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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

References

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

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HPK1 PROTAC C3

Biological Activity

Physicochemical Properties

References

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