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HPK1 PROTAC C3

Chemical Structure : HPK1 PROTAC C3

CAS No.:

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
Shipping
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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