1. Metabolic Enzyme/Protease
  2. Dihydroorotate Dehydrogenase
  3. hDHODH-IN-10

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。

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hDHODH-IN-10 Chemical Structure

hDHODH-IN-10 Chemical Structure

CAS No. : 3033087-05-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 values 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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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: LD50 is about 500 mg/kg.
Induced a weak dysfunction of liver.
分子量

470.80

Formula

C21H15ClF4N2O4

CAS 号
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.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
hDHODH-IN-10
目录号:
HY-151381
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