900897-56-5

KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf[1].

K-Ras WT: 0.28 μM (EC₅₀); KRAS(G12C): 0.63 μM (EC₅₀); KRas G12D: 0.37 μM (EC₅₀); KRas Q61H: 0.74 μM (EC₅₀)

[1] McCarthy MJ, et al. Discovery of High-Affinity Noncovalent Allosteric KRAS Inhibitors That Disrupt Effector Binding. ACS Omega. 2019 Feb 28;4(2):2921-2930. DOI:10.1021/acsomega.8b03308