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GNE-1858

Chemical Structure : GNE-1858

CAS No.: 2680616-96-8

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GNE-1858 (GNE1858)

Catalog No.: PC-72304Not For Human Use, Lab Use Only.

GNE-1858 (GNE1858) is a potent, selective, ATP-competitive inhibitor of HPK1 (MAP4K1) with IC50 of 1.9 nM in the SLP76 phosphorylation assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-1858 (GNE1858) is a potent, selective, ATP-competitive inhibitor of HPK1 (MAP4K1) with IC50 of 1.9 nM in the SLP76 phosphorylation assay.
GNE-1858 potently inhibits all three HPK1 kinase domain variants under investigation in a dose-dependent manner (IC50=4.5 nM against the residual kinase activity of HPK1-SA).

Physicochemical Properties

M.Wt 428.492
Formula C21H26F2N8
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

1H-Pyrazolo[4,3-c]pyridin-6-amine, N-[2-(3,3-difluoro-1-pyrrolidinyl)-6-(3-pyrrolidinyl)-4-pyrimidinyl]-1-(1-methylethyl)-

References

1. Wu P, et al. Structure. 2019 Jan 2;27(1):125-133.e4.

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