Benzamide, 2-(6-azaspiro[2.5]oct-6-yl)-N-[3-[[(1,1-dimethylethyl)amino]sulfonyl]phenyl]-4-[[(1-methylcyclopropyl)sulfonyl]amino]-

Biological Activity

KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1]. KIF18A-IN-3 (compound 24) exhibits a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours[1].Pharmacokinetic Parameters of KIF18A-IN-3 in female CD-1 mice[1]. IP (100 mg/kg) Cmax (μM)26.5AUC0-24 (μM.h)269 C24h (μM)0.8PPB (fu)0.015

References

[1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.