Chemical Structure : AZ3246
CAS No.:
2893978-54-4
AZ3246
(AZ-3246)
Catalog No.: PC-23939Not For Human Use, Lab Use Only.
AZ3246 is a potent, highly selective inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with IC50 of <3 nM in ADP-Glo assays, 20-fold more selective over GLK and no activity against LCK.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
AZ3246 is a potent, highly selective inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with IC50 of <3 nM in ADP-Glo assays, 20-fold more selective over GLK and no activity against LCK.
AZ3246 exhibits exquisite kinome selectivity: in a Thermo-Fisher kinase panel of 357 kinases, only HPK1 and MYLK at >80% inhibition at 100 nM.
AZ3246 induces IL-2 secretion in T cells with EC50 of 90 nM, without inhibiting antagonistic kinases.
AZ3246 is efficacious both as a monotherapy (30 mg/kg, b.i.d) and in combination with PD-L1 inhibition in an EMT6 mouse syngeneic model.
Physicochemical Properties
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M.Wt
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471.45
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Formula
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C21H20F3N9O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-Cyclopropyl-6-(3-methylimidazo[4,5-c]pyridin-7-yl)-3-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrazine-2-carboxamide
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References
1. Shields JD, et al. J Med Chem. 2025 Feb 10. doi: 10.1021/acs.jmedchem.4c02631.
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