| Identification | Back Directory | [Name]
2-[4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl]ethanol | [CAS]
900897-56-5 | [Synonyms]
KRAS inhibitor-3
KRAS inhibitor 11
1-Piperazineethanol, 4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-
2-[4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl]ethanol | [Molecular Formula]
C25H27N5O | [MOL File]
900897-56-5.mol | [Molecular Weight]
413.51 |
| Hazard Information | Back Directory | [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 (EC50); KRAS(G12C): 0.63 μM (EC50); KRas G12D: 0.37 μM (EC50); KRas Q61H: 0.74 μM (EC50) | [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 |
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