Pan KRas-IN-1 is a panKRasinhibitor, can be used for drug resistance incancerdeveloped with KRas G12C inhibitors^[1].

Pan KRas-IN-1 (example 5) shows high binding capacity to KRas, with IC₅₀s of<2 nm among different kras isform, including g12d, g12v, g12r, g12a, g12s, g13d, q61h, and wt^[1].
Pan KRas-IN-1 inhibits the phosphorylation of ERK downstream of KRas in different cells; AsPC-1 (G12D, IC₅₀=9 nM), A549 (G12S, IC₅₀=11 nM), HCT116 (G13D, IC₅₀=23 nM), NCI-H358 (G12C, IC₅₀=6 nM), NCI-H460 (Q61H, IC₅₀=12 nM), NCI-H727 (G12V, IC₅₀=29 nM), MKN1 (WT, IC₅₀=32 nM), PSN-1 (G12R, IC₅₀=681 nM)^[1].
Pan KRas-IN-1 (0-3000 nM; 5 d) exhibits anti-proliferative activity against mutation of reststance toAdagrasib(HY-130149, MRTX849) in mouse 3T3 fibroblasts, with IC₅₀s of 32 nM (G12A), 28.1 nM (G12C), 20.25 nM (G12D), 1742 nM (G12R), 94 nM (G12V), 50 nM (G12W), 610 nM (G13D), 58 nM (Q61H)^[1].

607.67

C₃₃H₃₆F₃N₅O₃

2791263-84-6

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