Description
An inhibitor of PI3Kα and PI3Kδ (IC50s = 6.2 and 5.7 nM, respectively); selective for PI3Kα and PI3Kδ over PI3Kβ and PI3Kγ (IC50s = 431 and 90 nM, respectively); inhibits Akt phosphorylation in PIK3CA constitutively active mutant BT474 cells and Jeko-1 B cells that express endogenous PI3Kδ (IC50s = 57 and 49 nM, respectively); reduces tumor growth and Akt phosphorylation in an SKOV3 mouse xenograft model at 25 mg/kg; increases the activity of CD8+ effector T cells and reduces tumor growth in a C26 mouse syngeneic tumor model
Formal name: 1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-pyrazinyl]-1-ethyl-1H-1,2,4-triazol-3-yl]-1-piperidinyl]-3-hydroxy-1-propanone
Synonyms:
Molecular weight: 469.5
CAS: 1620576-64-8
Purity: ≥98%
Formulation: A crystalline solid