KIF18A-IN-2

• CAT Number: I043855
• CAS Number: 2600559-20-2
• Molecular Formula: C25H34N4O5S2
• Molecular Weight: 534.69
• Purity: ≥95%
• Synonyms: 2-(6-azaspiro[2.5]octan-6-yl)-N-[3-(tert-butylsulfamoyl)phenyl]-4-(methanesulfonamido)benzamide
• InChI: InChI=1S/C25H34N4O5S2/c1-24(2,3)28-36(33,34)20-7-5-6-18(16-20)26-23(30)21-9-8-19(27-35(4,31)32)17-22(21)29-14-12-25(10-11-25)13-15-29/h5-9,16-17,27-28H,10-15H2,1-4H3,(H,26,30)
• InChIKey: BSVSZERUDCKTME-UHFFFAOYSA-N
• SMILES: CC(C)(C)NS(=O)(=O)C1=CC=CC(=C1)NC(=O)C2=C(C=C(C=C2)NS(=O)(=O)C)N3CCC4(CC4)CC3

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)
12.6

AUC0-24 (μM·h)
147

C24h (μM)
2.9

PPB (fu)
0.007

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.
 [Content Brief]