KIF18A-IN-2

KIF18A-IN-2 is a potent KIF18A inhibitor (IC50=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

IC50: 28 nM (KIF18A)[1]

KIF18A-IN-2 (compound 23) (100 mg/kg; i.p., single) 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-2 in female CD-1 mice[1]. IP (100 mg/kg) Cmax (μM) 12.6 AUC0-24 (μM·h) 147 C24h (μM) 2.9 PPB (fu) 0.007 Animal Model: Female athymic nude mice (4-7 weeks; injected with human OVCAR-3 HGSOC cells)[1] Dosage: 100 mg/kg Administration: i.p., single Result: Showed a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours.

[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.