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编 号:F762799
分子式:C21H15ClF4N2O4
分子量:470.8
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生物活性:
hDHODH-IN-10 is a selective, potent and orally active hDHODH inhibitor, with an IC50 value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation of cancer cells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectal cancer.

体内研究:
hDHODH-IN-10 (compound 7d, 30 mg/kg, oral administration) inhibits tumor growth in Raji and HCT116 cells xenograft mice model.hDHODH-IN-10 (500 mg/kg, oral administration) exhibits a favorable safety profile.Animal Model:Raji and HCT116 cells xenograft mice model
Dosage:30 mg/kg
Administration:Oral administration
Result:Showed a tumor growth inhibitory (TGI) rate of 58.3% (Raji model) and 42.1% (HCT116 model).
Animal Model:BALB/c mice (acute toxicity assay)
Dosage:500 mg/kg
Administration:Oral administration
Result:LD50 is about 500 mg/kg.Induced a weak dysfunction of liver.

体外研究:
hDHODH-IN-10 (compound 7d, 1 nM-100 μM) displays anti-proliferative activities against multiple human cancer cells.hDHODH-IN-10 (0.0625-0.25 μM, 24 h) increases the percentage of S-phase cells in Raji and HCT116 cells.
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