1455031-68-1

LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation[1][2].

[1] Yao YM, et al. Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. DOI:10.1158/1078-0432.CCR-16-3250
[2] Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017.