raf mutant-in-1

RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively).

Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor used in treating proliferative diseases characterized by activating mutations in the MAPK pathway, particularly KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC), and KRAS-mutant ovarian cancer[1].

Pan-RAS-IN-2 (compound 6A) is an orally active molecular glue that targets RAS by inducing ternary complex formation with cyclophilin A (CYPA) and RAS in the ON state, leading to potent inhibition of downstream RAF binding and pERK signaling with an IC50 of 0.3 nM in AsPC-1 cells, Pan-RAS-IN-2 demonstrates strong antiproliferative effects in RAS-mutant cancer cell lines, supporting research into targeted therapies for colorectal and pancreatic cancers.