KS16

KS16 is a small molecule RAF kinase inhibitor featuring an imidazothiazole core scaffold, designed to target a selective back pocket in the active site of RAF kinases. This mechanism is intended to overcome resistance to standard BRAF inhibitors like vemurafenib and dabrafenib, which often occurs via CRAF activation. In preclinical studies, KS16 demonstrated potent inhibition of mutated BRAF (V600E), wild-type BRAF, and CRAF, and showed selective cytotoxicity against melanoma cell lines, including resistant A375R cells. It also exhibits a favorable cardiac safety profile with weak hERG channel binding. The compound was developed through a multi-institutional collaboration including the Korea Institute of Science and Technology (KIST) and CTCBIO Inc.