| Identification | Back Directory | [Name]
Benzamide, 2-(6-azaspiro[2.5]oct-6-yl)-N-[3-[[(1,1-dimethylethyl)amino]sulfonyl]phenyl]-4-[[(1-methylcyclopropyl)sulfonyl]amino]- | [CAS]
2600577-49-7 | [Synonyms]
KIF18A-IN-3
Benzamide, 2-(6-azaspiro[2.5]oct-6-yl)-N-[3-[[(1,1-dimethylethyl)amino]sulfonyl]phenyl]-4-[[(1-methylcyclopropyl)sulfonyl]amino]- | [Molecular Formula]
C28H38N4O5S2 | [MOL File]
2600577-49-7.mol | [Molecular Weight]
574.76 |
| Hazard Information | Back Directory | [Uses]
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]. | [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 | [in vivo]
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. |
| [storage]
Store at -20°C | [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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