Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 6-fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid, monosodium salt
Purity: ≥98%
Formula Markup: C23H14F2NO2 / Na
Formula Weight: 397.4
CAS Number: 96201-88-6
Notes: 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 (EC50s = ~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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