In vivo, NMS-1286937 administered at 45 mg/kg intravenously results in significant tumor growth inhibition with tolerable and reversible weight loss in CD1 nu/nu mice xenografted with HCT116 colon adenocarcinoma cells. Oral administration of the compound at 60 mg/kg also effectively inhibits tumor growth in the HCT116 xenograft model^[1].

The efficacy of NMS-P937, either at 45 mg/kg intravenously or 60 mg/kg orally, is comparable, showing tumor growth inhibition (TGI) rates of 83% and 79%, respectively, in mice harboring HCT116 tumors. The combination therapy involving NMS-P937 (120 mg/kg administered in four cycles of two consecutive days followed by a 10-day rest period) and cytarabine (75 mg/kg administered in four cycles of five consecutive days followed by a 7-day rest period) in a disseminated leukemia model (AmL-PS) is well tolerated and significantly enhances survival^[2].

Moreover, NMS-P937 at a dosage of 60 mg/kg administered twice daily over two days with a 5-day rest period showcases superior efficacy compared to standard therapies, markedly extending the median survival time (MST) in established disease settings^[3].

NMS-1286937 is a potent, selective, and orally available inhibitor of Polo-like kinase 1 (PLK1), boasting an IC50 of 2 nM. This compound also exhibits inhibitory effects on FLT3, MELK, and CK2 with IC50 values of 510, 744, and 826 nM, respectively^[1].

NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. At a concentration of 10 μM, NMS-P937 (another name for NMS-1286937) demonstrates selectivity with only marginal activity, inhibiting PLK2 and PLK3 by 48% and 40%, respectively. It displays antiproliferative effects against a wide array of cell lines, achieving IC50 values below 100 nM in 60 out of 137 tested cell lines, with only 9 cell lines exhibiting IC50 values higher than 1 μM^[2].

NMS-P937 shows notable cytotoxic activity against AmL-NS8 cells with an IC50 of 36 nM^[3].