CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10?6 cm/s[1].
| Animal Model: | CT-26 xenograft mice[1] |
| Dosage: | 10 and 40 mg/kg |
| Administration: | Oral adminstration (p.o.) |
| Result: | Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor. |
| Animal Model: | Rats (pharmacokinetic assay)[1] |
| Dosage: | 10 mg/kg (p.o.), 2 mg/kg (i.v.) |
| Administration: | Oral adminstration (p.o.) or intravenous injection (i.v.) |
| Result: | Pharmacokinetic profile of CDK8-IN-11 (compound 29).
| dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | F (%) | |
| 10 (p.o.) | 1.1 | 0.8 | 453 | 31.7 | |
| 2 (i.v.) | 0.5 | | 318 | |
|