Uses
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].
IC 50
K-Ras WT: 0.28 μM (EC
50); KRAS(G12C): 0.63 μM (EC
50); KRas G12D: 0.37 μM (EC
50); KRas Q61H: 0.74 μM (EC
50)
References
[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
![2-[4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl]ethanol Structure](https://www.chemicalbook.com/CAS/20180719/GIF/900897-56-5.gif)
