TAK-733

TAK-733 is a potent and selective investigational small molecule inhibitor of MEK1 and MEK2 (mitogen‑activated protein kinase kinases), acting as a non‑ATP competitive allosteric inhibitor. It was developed as an antineoplastic agent for the treatment of various advanced solid tumors including melanoma and colorectal cancer. Preclinical studies demonstrated robust antitumor activity in cell lines and xenograft models with KRAS or BRAF mutations. In clinical trials, it showed pharmacodynamic evidence of ERK pathway inhibition but limited single-agent efficacy in patients with advanced solid tumors. The drug was administered orally and exhibited manageable toxicity up to the maximum tolerated dose; however, further development has been discontinued[1][6][8].

Other names

(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione1035555-63-5UNII-5J61HSP0QJUNII5J61HSP0QJUNII 5J61HSP0QJ