Description
An inhibitor of DNA-PK (IC50 = 0.63 nM in an enzyme assay); selective for DNA-PK over TTK (IC50 = 5.012 μM), as well as JAK1, JAK2, JAK3, Aurora A, and Aurora B (IC50s = >10 μM for all); reduces tumor growth in a FaDu ATM KO pharynx cancer mouse xenograft model at 37.5 or 75 mg/kg twice per day and induces tumor regression at these doses when administered in combination with the PARP inhibitor olaparib
Formal name: 7,9-dihydro-7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-8H-purin-8-one
Synonyms:
Molecular weight: 380.4
CAS: 2230820-11-6
Purity: ≥98%
Formulation: A crystalline solid