Catalog No.: PC-26712Not For Human Use, Lab Use Only.
BLU2864 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 0.3 nM and Kd of 3.3 nM.
BLU2864 is a potent, selective and orally acitve protein kinase A (PKA) alpha catalytic subunit (PRKACA) inhibitor with IC50 of 0.3 nM and Kd of 3.3 nM. BLU2864 exhibits good to moderate selectivity against closely related AGC kinase family members and excellent overall kinome selectivity profiles. BLU2864 exhibits cellular IC50 value of 36.6 nM for inhibition of VASP Ser157 phosphorylation in forskolin-stimulated Huh7 cells. BLU2864 treatment led to a dose-dependent reduction in phosphorylated VASP in FLC PDX spheroid cultures. BLU2864 at 30 mg/kg once daily (QD) inhibits PRKACA in vivo, inhibits tumor growth in mice harboring FLC PDX tumors.
