Catalog No.: PC-27366Not For Human Use, Lab Use Only.
AM-2383 is a potent, selective pan-KRAS inhibitor that blocks signaling via both the GDP(off)- and GTP(on)-bound states of KRAS, potently bind to a diverse set of common oncogenic KRAS mutants with IC50 of 2-10 nM in NanoBRET KRAS target engagement assay, also potently bind to KRAS WT (IC50=2 nM).
AM-2383 is a potent, selective pan-KRAS inhibitor that blocks signaling via both the GDP(off)- and GTP(on)-bound states of KRAS, potently bind to a diverse set of common oncogenic KRAS mutants with IC50 of 2-10 nM in NanoBRET KRAS target engagement assay, also potently bind to KRAS WT (IC50=2 nM). AM-2383 shows little activity toward related RAS isoforms (HRAS Coupled Exchange Activity IC50 = 0.320 (>80-fold selectivity); NRAS Coupled Exchange Activity IC50 = 1.60 μM (>400-fold selectivity). AM-2383 binds to KRAS WT with a KD value of 0.03 nM, with much weaker affinity for HRAS and NRAS with a KD value of 139 nM and 2.6 uM. AM-2383 potently inhibits ERK phosphorylation across common KRAS mutants (G12D, G12V, & G12C; IC50 = 3-9 nM) across KRAS mutant cell lines. AM-2383 showsrobust antiproliferative activity (avg. IC50 = 30 nM) across KRAS mutant cell lines, does not impact proliferation in KRASWT or NRAS mutant cell lines. AM-2383 (100 mg/kg, QD, oral) induces 80% tumor growth inhibition (TGI) in AsPC-1 tumor xenograft model.
