For research use only. Not for therapeutic Use.
HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs)[1].
HPK1-IN-3 (compound 27; 0.25-4 μM; 24-h) treatment shows a statistically significant elevation of proinflammatory cytokines IL-6 and TNF-α was observed in a concentration-dependent manner in human monocyte-derived dendritic cells[1].
| Catalog Number | I044615 |
| CAS Number | 2739844-34-7 |
| Synonyms | 4-[2-fluoro-6-(trifluoromethyl)anilino]-2-[(6-methoxy-2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)amino]pyrimidine-5-carboxamide |
| Molecular Formula | C23H22F4N6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H22F4N6O2/c1-33-7-6-12-9-18(35-2)17(8-13(12)11-33)30-22-29-10-14(20(28)34)21(32-22)31-19-15(23(25,26)27)4-3-5-16(19)24/h3-5,8-10H,6-7,11H2,1-2H3,(H2,28,34)(H2,29,30,31,32) |
| InChIKey | RZLXOEIALAVGKH-UHFFFAOYSA-N |
| SMILES | CN1CCC2=CC(=C(C=C2C1)NC3=NC=C(C(=N3)NC4=C(C=CC=C4F)C(F)(F)F)C(=O)N)OC |
| Reference | [1]. Brandon A Vara, et al. Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds. ACS Med Chem Lett. 2021 Mar 19;12(4):653-661. |
