产品
编 号:F230106
分子式:C30H36Br2N4O2
分子量:644.44
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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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50mg
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生物活性:
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.

体内研究:
EB-3D (1 mg/kg; i.p.; every other day) impairs mammary tumor growth in syngeneic orthotopic E0771-C57BL/6 mouse model.EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis.Animal Model:E0771-C57BL/6 mice
Dosage:I.p.; every other day for 4 weeks
Administration:2.5 mg/kg
Result:A reduction of the number of spontaneous lung macro- and micrometastasis.

体外研究:
EB-3D displays (0-100 μM; 72 hours) excellent antiproliferative activity against a wide cohort of T-leukemic cell lines, with GI GI50s 13 values in the nanomolar range.EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines.EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis.EB-3D (0.3 μM; 48 hours) shows a first spike of activation of AMPKα after 30 minutes and a later increase in the phosphorylation of T172.EB-3D (1-40 μM; 48?hours) inhibits cell growth in HepG2 cells with a GI50 of 14.55 μM.EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
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