2695505-82-7

RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAFwt, and bRAFV600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAFV600E mutation, respectively[1].

BRaf^V600E: 29.4 nM (IC₅₀); BRAF^WT: 36 nM (IC₅₀); c-Raf: 3.8 nM (IC₅₀)

[1] Zhao P, et al. Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers. Eur J Med Chem. 2022;228:114040. DOI:10.1016/j.ejmech.2021.114040