KIF18A-IN-3

• CAT Number: I043854
• CAS Number: 2600577-49-7
• Molecular Formula: C28H38N4O5S2
• Molecular Weight: 574.76
• Purity: ≥95%
• Synonyms: 2-(6-azaspiro[2.5]octan-6-yl)-N-[3-(tert-butylsulfamoyl)phenyl]-4-[(1-methylcyclopropyl)sulfonylamino]benzamide
• InChI: InChI=1S/C28H38N4O5S2/c1-26(2,3)31-38(34,35)22-7-5-6-20(18-22)29-25(33)23-9-8-21(30-39(36,37)27(4)10-11-27)19-24(23)32-16-14-28(12-13-28)15-17-32/h5-9,18-19,30-31H,10-17H2,1-4H3,(H,29,33)
• InChIKey: MZGYQJDGUVDYIK-UHFFFAOYSA-N
• SMILES: CC1(CC1)S(=O)(=O)NC2=CC(=C(C=C2)C(=O)NC3=CC(=CC=C3)S(=O)(=O)NC(C)(C)C)N4CCC5(CC5)CC4

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)
26.5

AUC0-24 (μM·h)
269

C24h (μM)
0.8

PPB (fu)
0.015

Reference

[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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