| Identification | Back Directory | [Name]
Benzamide, 2-(6-azaspiro[2.5]oct-6-yl)-N-[3-[[(1,1-dimethylethyl)amino]sulfonyl]phenyl]-4-[(methylsulfonyl)amino]- | [CAS]
2600559-20-2 | [Synonyms]
KIF18A-IN-2
Benzamide, 2-(6-azaspiro[2.5]oct-6-yl)-N-[3-[[(1,1-dimethylethyl)amino]sulfonyl]phenyl]-4-[(methylsulfonyl)amino]- | [Molecular Formula]
C25H34N4O5S2 | [MOL File]
2600559-20-2.mol | [Molecular Weight]
534.69 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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)12.6AUC0-24 (μM.h)147 C24h (μM)2.9PPB (fu)0.007 | [in vivo]
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. |
| [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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