AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.
AM-1882 exhibits good specificity against a panel of diverse kinesin motor proteins, except for the KIF19A motor (IC50=1820 nM).
AM-1882 shows cellular EC50 of 21 and 15 nM for cell line pH3+ and PCM foci in mitotic image assays respectively.
AM-1882 has similar inhibitory effects on the motor activity of human and mouse KIF18A.
AM-1882 is active in a subset of cancer cell lines with CCNE1, BRCA1 and RB1 gene alterations and can enhance apoptosis when combined with PARP inhibition.
AM-1882 (50 or 100 mg per kg, i.p.) inhibited tumor growth in OVCAR-8 CDX tumor model.
