Name | c-Kit-IN-3 |
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). |
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 100 mg/mL (193.46 mM)
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Keywords | c-Kit-IN-3 | cKitIN3 | c Kit IN 3 |
Inhibitors Related | Gilteritinib | Regorafenib monohydrate | Imatinib Mesylate | Sorafenib | Pexidartinib | Dasatinib | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate | Imatinib | Pazopanib | Axitinib |
Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Hematonosis Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library |