BLU0588 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 1 nM and Kd of 4 nM.
BLU0588 exhibits good to moderate selectivity against closely related AGC kinase family members and excellent overall kinome selectivity profiles.
BLU0588 exhibits cellular IC50 value of 25.0 nM for inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells.
BLU0588 treatment led to a dose-dependent reduction in phosphorylated VASP in FLC PDX spheroid cultures.
BLU0588 at 30 mg/kg and 75 mg/kg once daily (QD) inhibits PRKACA in vivo, inhibits tumor growth in mice harboring FLC PDX tumors.
