AZ3246 | HPK1 inhibitor | Probechem Biochemicals

Chemical Structure : AZ3246

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AZ3246 (AZ-3246)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	471.45
分子式	C21H20F3N9O
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
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Shields JD, et al. J Med Chem. 2025 Feb 10. doi: 10.1021/acs.jmedchem.4c02631.

AZ3246 (AZ-3246)

生物&药学活性

物理化学性质&存储条件

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AZ3246 (AZ-3246)

生物&药学活性

物理化学性质&存储条件

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