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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $79 | In Stock | |
5 mg | $165 | In Stock | |
10 mg | $267 | In Stock | |
25 mg | $441 | In Stock | |
50 mg | $592 | In Stock | |
100 mg | $828 | In Stock | |
500 mg | $1,660 | In Stock | |
1 mL x 10 mM (in DMSO) | $352 | In Stock |
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 (WT):4 nM , c-Kit (T670I):8 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (193.46 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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