IC50: 9.4 nM (KIF18A microtubule-dependent ATPase activity)[1]
KIF18A-IN-7 (Compound 22) is an orally active KIF18A inhibitor with an IC50 of 9.4 nM against KIF18A microtubule-dependent ATPase activity[1].
KIF18A-IN-7 (Compound 22; 7 days) 抑制 JIMT-1、NIH-OVCAR3 和 HCC-15 细胞活力，IC50 分别为 0.0078、0.0097 和 0.011 μM[1]。
Cell Viability Assay[1]
| Cell Line: | HCC-15, JIMT-1 and NIH-OVCAR3 |
| Concentration: | |
| Incubation Time: | 7 days |
| Result: | Inhibited cell viability with IC50s of 0.0078, 0.0097 and 0.011 μM against JIMT-1, NIH-OVCAR3 and HCC-15 cells, respectively. |
KIF18A-IN-7 (Compound 22; 10-60 mg/kg; p.o.; twice or once a day for 1 month) 抑制小鼠 HCC15 和 OVCAR3 肿瘤生长[1]。
| Animal Model: | SCID Beige mice, HCC15 tumor model[1] |
| Dosage: | 10, 30 and 60 mg/kg |
| Administration: | PO, twice a day for 1 month |
| Result: | Inhibited tumor growth by 30±15%, 72±6% and 82±9% at 10, 30 and 60 mg/kg, respectively. |
| Animal Model: | Balb/C nude mice, OVCAR3 tumor model[1] |
| Dosage: | 10, 30 and 60 mg/kg |
| Administration: | PO, once a day for 1 month |
| Result: | Inhibited tumor growth by 24±26%, 72±17% and 82±10% at 10, 30 and 60 mg/kg, respectively. |
[1]. COGAN, et al. SPIRO INDOLINE INHIBITORS OF KIF18A. Patent WO2023028564.