Pan-rasin-2 (compound 6A) is an orally active molecular glues that targets RAS. Pan-RAS-IN-2 inhibits pERK (IC50 in AsPC-1 cells: 0.3 nM). Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor (such as colorectal cancer, pancreatic cancer) effects.
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