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) 26.5 AUC0-24 (μM·h) 269 C24h (μM) 0.8 PPB (fu) 0.015 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.
In Vitro
Kinase Assay
Cell Assay
Animal Administration
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.
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