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编 号:F618333
分子式:C25H34FN7O
分子量:467.58
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1mg
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5mg
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生物活性:
JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

体内研究:
JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects.Animal Model:NOD/SCID mouse models
Dosage:30 and 60 mg/kg
Administration:Oral administration; daily; for 14 days
Result:Exhibited significant antitumor effects.The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

体外研究:
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner.JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells.
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