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编 号:F115189
分子式:C18H24N2O3S
分子量:348.46
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生物活性:
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.

体内研究:
K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice.Animal Model:BALB/c-nu mice injected with U937 cells
Dosage:50 mg/kg
Administration:Oral gavage; daily; for 15 days
Result:Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

体外研究:
K145 (0-10 μM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.K145 (10 μM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells.K145 (4-8 μM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.Treatment with K145 (10 μM) causes a decrease of total cellular S1P without significant effects on ceramide levels.
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