Catalog No.: PC-23305Not For Human Use, Lab Use Only.
pan-KRAS degrader 4 is a potent, selective, reversible heterobifunctional pan-KRAS PROTAC degrader with Dmax50 of 17 nM in GP5d cells, efficiently degrades 13 of the 17 most prevalent KRAS mutant alleles and KRASWT with single-digit nanomolar potency.
pan-KRAS degrader 4 is a potent, selective, reversible heterobifunctional pan-KRAS PROTAC degrader with Dmax50 of 17 nM in GP5d cells, efficiently degrades 13 of the 17 most prevalent KRAS mutant alleles and KRASWT with single-digit nanomolar potency. pan-KRAS degrader 4 exhibits potent cellular VHL-dependent degradation for endogenous KRASG12D (GP5d, DC50=1 nM, Dmax=99.5%) and KRASG12V (SW620, DC50=13 nM, Dmax=89%). pan-KRAS degrader 4 less potently degrades KRASG12R (DC50=45 nM, Dmax=59%) and KRAS Q61L/K/R (DC50 > 470 nM, Dmax < 60%) in cell lines expressing KRASG12S, KRASG12A, KRASG13D, and KRASQ61H. pan-KRAS degrader 4 impacts MAPK signaling and cancer cell proliferation, suppresses pERK and DUSP6, inhibits sotorasib-sensitive KRASG12C-mutant cell lines. pan-KRAS degrader 4 exhibits in vivo DC50 of 851 nM for the GP2d model in NMRI mice (versus 3.6 nM in 10% FCS).
