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编 号:F156530
分子式:C18H15N3O2
分子量:305.33
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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:
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.

体内研究:
GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells.GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model.Animal Model:Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells
Dosage:10 mg/kg
Administration:Oral gavage
Result:Reduced both proneural and mesenchymal markers.
Animal Model:Subcutaneous colorectal cancer model (HCT116)
Dosage:5 mg/kg
Administration:Tail vein injection, twice a week
Result:Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.

体外研究:
GN44028 (compound 2I, 0-30 μM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells.GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells.GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells.
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