hDHODH-IN-10 是一种有效的、选择性的、具有口服活性的hDHODH抑制剂，IC50值为 10.9 nM。hDHODH-IN-10 与关键残基 Arg136 和 Gln47 形成氢键。hDHODH-IN-10 可抑制癌细胞的增殖。hDHODH-IN-10 可用于癌症研究，如 AML、结肠癌。
| 生物活性 | hDHODH-IN-10 is a selective, potent and orally activehDHODHinhibitor, with anIC50value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation ofcancercells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectalcancer[1]. |
| IC50& Target | IC50: hDHODH (10.9 nM)[1]. |
体外研究
(In Vitro) | hDHODH-IN-10 (compound 7d, 1 nM-100 μM) displays anti-proliferative activities against multiple human cancer cells[1].
hDHODH-IN-10 (0.0625-0.25 μM, 24 h) increases the percentage of S-phase cells in Raji and HCT116 cells[1].
Cell Viability Assay[1] | Cell Line: | U937, HCT116, A375, Kasumi-1 and KG-1 cells | | Concentration: | 0-10 μM approximately | | Incubation Time: | 96 h | | Result: | Inhibits cell proliferation with IC50values of 0.1-0.8 μM. |
Cell Cycle Analysis[1] | Cell Line: | Raji and HCT116 cells | | Concentration: | 0.0625, 0.125 and 0.25 μM | | Incubation Time: | 24 h | | Result: | Increased the percentage of S-phase cells from 42.8% to 54.2%, 60.6% and 67.1%, respectively. |
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体内研究
(In Vivo) | hDHODH-IN-10 (compound 7d, 30 mg/kg, oral administration) inhibits tumor growth in Raji and HCT116 cells xenograft mice model[1].
hDHODH-IN-10 (500 mg/kg, oral administration) exhibits a favorable safety profile[1].
| Animal Model: | Raji and HCT116 cells xenograft mice model[1] | | 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)[1] | | Dosage: | 500 mg/kg | | Administration: | Oral administration | | Result: | LD50is about 500 mg/kg.
Induced a weak dysfunction of liver. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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