A DHODH inhibitor (IC50 = ~20 nM); selective for DHODH over a panel of greater than 400 kinases at 100 nM; induces differentiation of ER-HoxA9

Brequinar – 10 mg

Brand:
Cayman
CAS:
96187-53-0
Storage:
-20
UN-No:
Non-Hazardous - /

Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH; IC50 = ~20 nM), the enzyme that converts dihydroorotate to orotate during de novo pyrimidine synthesis.{39048} Brequinar is selective for DHODH over a panel of greater than 400 kinases at 100 nM. It induces differentiation of ER-HoxA9, U937, and THP-1 cells in vitro (ED50s = ~1 µM) and of tumor cells in a THP-1 mouse xenograft model when administered at doses of 15 mg/kg three times daily and 5 mg/kg per day. It also reduces tumor growth in THP-1, HL-60, and MOLM-13 mouse xenograft models. In a retroviral transduction mouse model of HoxA9 + Meis1 acute myeloid leukemia (AML), brequinar induces differentiation of bone marrow leukemic cells and increases survival.  

 

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Description

A DHODH inhibitor (IC50 = ~20 nM); selective for DHODH over a panel of greater than 400 kinases at 100 nM; induces differentiation of ER-HoxA9, U937, and THP-1 cells in vitro (ED50s = ~1 µM); induces differentiation of tumor cells and reduces tumor growth in a THP-1 mouse xenograft model at 15 mg/kg three times daily or 5 mg/kg per day; induces differentiation of bone marrow leukemic cells and increases survival In a retroviral transduction mouse model of HoxA9 + Meis1 AML

Formal name: 6-fluoro-2-(2′-fluoro[1,1′-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid

Synonyms:  NSC 368390

Molecular weight: 375.4

CAS: 96187-53-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer

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