化学性质：                                                                                                             

产品描述：                                                                                                            

Potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor (IC50 = ~20 nM). Causes depletion of pyrimidine nucleotides. Exhibits minimal inhibition against a panel of >400 kinases. Triggers differentiation of AML cell lines (ED50 = ~ 1 μM. Note uridine concentration effects ED50 value). Causes differentiation and depletion of leukemia-initiating cells in vivo. Antimetabolite.

Arteaga (1989) Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390). Cancer Res. 49 4648 PMID:2743343 |Sykes et al (2016) Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia. Cell 167 171 PMID:27641501 |Peters et al (1987) Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390). Invest.New Drugs 5 235 PMID:2822596

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