MedKoo product information:

  NMS1286937

Description of NMS1286937: NMS1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor NMS-1286937 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Nerviano Medical Sciences.

Preclinical evaluation has shown high potency of the compound in proliferation assays, displaying low nanomolar activity on a large number of cell lines, representative of both solid and hematological tumors. NMS-1286937 potently causes a mitotic cell cycle arrest followed by apoptosis in cancer cell lines and it inhibits xenograft tumor growth with demonstrated PLK1-related mechanism of action, after oral administration. NMS-1286937 also shows potential for combination with approved cytotoxic drugs in various clinical settings, causing tumor regression in xenograft models. Currently a phase I trial evaluating NMS-1286937 for the treatment of solid tumors is ongoing. (source: http://www.nervianoms.com/en/oncology-en/pipeline/nms-1286937.html).