Description
| Description | c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I). |
| Targets&IC50 | c-Kit (T670I):8 nM , c-Kit (WT):4 nM |
| In vitro | In primary GIST patient cells, c-Kit-IN-3 (0.1-10 μM) exhibits dose-dependent antiproliferative effects. In GIST-T1, GIST-T1-T670I, and GIST-5R cells, c-Kit-IN-3 (0.01-1 μM) induces dose-dependent cell apoptotic death and arrests the cell cycle into the G0/G1 phase[1]. |
| In vivo | c-Kit-IN-3 (1 mg/kg i.v. for mice, rats, dog; 10 mg/kg p.o. for mice, rats; 5 mg/kg p.o. for dog) has T1/2 of 4.5 h, 6.4 h, 19.4 h for mice, rats and dogs, respectively. c-Kit-IN-3 possesses acceptable bioavailability of 43%, 50% and 81% for mice, rats, and dogs. In female BALB/C-nu mice, c-Kit-IN-3 (20-100 mg/kg; gavage) treatment dose-dependently inhibits the tumor progression[1]. |
| Molecular Weight |
516.9 |
| Formula | C26H20ClF3N2O4 |
| CAS No. | 2363169-01-9 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 100 mg/mL (193.46 mM)
