c-Kit-IN-3 是 c-Kit 激酶的特异性抑制剂，对 c-Kit (wt) 和 c-Kit (T670I) 的 IC50 分别为 4 nM、8 nM。

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).

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].

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].

2363169-01-9

C26H20ClF3N2O4

516.9

DMSO:100 mg/mL (193.46 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years