产品
编 号:F002048
分子式:C23H17N5O2
分子量:395.41
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties.

体内研究:
c-Kit-IN-5 (compound 25) (1 mg/kg; i.v.) exhibits CL (0.46 L/h/kg) and Vdss (1.59 L/kg) in rats.c-Kit-IN-5 (10 mg/kg; p.o.) exhibits AUC0-t(9860 ng?h/mL) Cmax(1230 ng/mL), T1/2 (2.6 h), and F (39%) in rats.

体外研究:
c-Kit-IN-5 (compound 25) shows more than 200-fold selectivity against KDR, p38, Lck, and Src (IC50=>5.0, 40, 7.8 , and >5.0 μM, respectively).
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