RP-1664 (RP1664) is potent, selective and orally available inhibitor of PLK4 with IC50 of 3 nM, >1900-fold selective over Aurora A/B.
RP-1664 has EC50 of 0.13 uM in PLK4 centriole depletion assay definition (CDA), and EC50 of 0.051 uM for viability assay in MCF7 cells
RP-1664 binds PLK4 with 59-fold selectivity over FAK and 3-fold selectivity over TNK1 in NanoBRET assays.
RP-1664 potently inhibits TRIM37-high cell lines with IC50 of 80 and 26 nM in cell growth assays, respectively, for CAL-148 and TRIM37 gain-carrying neuroblastoma CHP-134 cells.
RP-1664 (6, 11, and 21 mg/kg PO BID) demonstrates responsive tumor growth inhibition, stasis and regressionsin CAL-148 breast and CHP-134 neuroblastoma model.
