IC50: 0.016 μM (KIF18A microtubule-dependent ATPase activity)[1]
KIF18A-IN-6 (Compound 134) is an orally active KIF18A inhibitor with an IC50 of 0.016 μM against KIF18A microtubule-dependent ATPase activity[1].
KIF18A-IN-6 (Compound 134; 7 days) 抑制 JIMT-1、HCC-15 和 NIH-OVCAR3 细胞活力，IC50 分别为 0.0040、0.0051 和 0.0051 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 0.0040, 0.0051 and 0.0051 μM against JIMT-1, HCC-15 and NIH-OVCAR3 cells, respectively. |
KIF18A-IN-6 (Compound 134; 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 61±10%, 89±7% and 94±5% 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, twice or once a day for 1 month |
| Result: | Completely inhibited tumor growth (over 100%) over 30 mg/kg. |
[1]. COGAN, et al. SPIRO INDOLINE INHIBITORS OF KIF18A. Patent WO2023028564.