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Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect[1]. | [IC 50]
TrkA: 0.33 μM (IC50); CDK2: 0.71 μM (IC50); CK2: 0.09 μM (IC50); PIM1: 0.42 μM (IC50); Chk1: 0.15 μM (IC50); EGFR: 0.1 μM (IC50); c-KIT: 0.05 μM (IC50); ALK2: 0.03 μM (IC50); RET: 0.53 μM (IC50); FLT3: 0.34 μM (IC50); ROS1: 0.75 μM (IC50) | [References]
[1] Mustafa A. Al-Qadhi, et al. Design and synthesis of certain 7-Aryl-2-Methyl-3-Substituted Pyrazolo{1,5-a}Pyrimidines as multikinase inhibitors. European Journal of Medicinal Chemistry. Volume 262, 15 December 2023, 115918. |
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