Brequinar

Brequinar

CAT N°: 24445
Price:

From 48.00 40.80

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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 6-fluoro-2-(2′-fluoro[1,1′-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid
  • Correlated keywords
    • BPQ ERHoxA9 ERHox A9 U-937 THP1 HL60 MOLM13 HOXA-9 Meis-1 NSC368390 BRQ Biphenquinate 96201-88-6
  • Product Overview:
    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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