PF-3758309 is a thienopyrimidine containing a thieno[3,2-d]pyrimidine core substituted at positions 2 and 4 with a methyl group and a (5-{[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl}-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)amino group, respectively. It is a potent PAK4 inhibitor that suppresses the growth of multiple human tumor xenografts. It functions as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor, an apoptosis inducer, and an antineoplastic agent. It is classified as a thienopyrimidine, pyrrolopyrazole, benzene derivative, urea, secondary amino compound, and tertiary amino compound.
