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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
471.45
|
|
Formula
|
C21H20F3N9O
|
|
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
|
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
|
References
1. Shields JD, et al. J Med Chem. 2025 Feb 10. doi: 10.1021/acs.jmedchem.4c02631.
Contact Us
sales@probechem.com
