ci-1040

CI-1040 is an orally active, highly specific small-molecule inhibitor of mitogen‑activated protein kinase kinases 1 and 2 (MEK1/MEK2), which are key components of the MAPK/ERK signaling pathway. By inhibiting MEK1/MEK2, CI‑1040 blocks phosphorylation and activation of ERK1/ERK2, thereby suppressing downstream signal transduction involved in cell proliferation and survival. This mechanism targets tumor growth driven by aberrant MAP kinase pathway activation. Developed as an anticancer agent, CI‑1040 was the first MEK inhibitor to enter clinical trials and has been evaluated in phase I studies for advanced malignancies including lung cancer, breast cancer, pancreatic cancer, colorectal cancer, and other solid tumors. While it demonstrated target inhibition and some antitumor activity (notably a partial response in pancreatic cancer), its development was ultimately discontinued due to limited efficacy[1][3][4][5].

Other names

2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamideR3K9Y00J04R-3K9Y00J04R 3K9Y00J04