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

hDHODH-IN-10 

Cat. No.: HY-151381
Handling Instructions

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.

For research use only. We do not sell to patients.

hDHODH-IN-10 Chemical Structure

hDHODH-IN-10 Chemical Structure

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Description

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].

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.
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.
Molecular Weight

470.80

Formula

C21H15ClF4N2O4

SMILES

C/C(O)=C(C(NC1=C(C=C(C(O[[email protected]](C(F)(F)F)C)=C1)C(C2=C(C=CC=C2)Cl)=O)F)=O)\C#N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
hDHODH-IN-10
Cat. No.:
HY-151381
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