MK-5108

MK-5108 is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A. It competitively binds to the ATP binding site of Aurora A kinase, resulting in potent inhibition (IC50 = 0.064 nM) and high selectivity over Aurora B and C kinases[1][2][4][7]. By inhibiting Aurora A kinase, which regulates mitotic spindle assembly and chromosome segregation during cell division, MK-5108 disrupts mitosis leading to cell cycle arrest and apoptosis in cancer cells that overexpress this target[1]. The drug has demonstrated antitumor activity across a range of solid tumor types in preclinical models. Developed initially by Vertex Pharmaceuticals as VX‑689 and later licensed to Merck, it advanced into phase I clinical trials for advanced or refractory solid tumors both as monotherapy and in combination with docetaxel; however, development was terminated early due to toxicities at doses below anticipated exposure targets[5][6][8].

Other names

1010085-13-8H8J407531SH-8J407531SH 8J407531S