AG-636

AG-636 is a dihydroorotate dehydrogenase (DHODH) inhibitor (IC50 = 17 nM). It increases levels of ureidosuccinic acid (Cay-34126) and DHO, pyrimidine biosynthesis metabolites upstream of DHODH, in a panel of six cell lines when used at a concentration of 1 µM. AG-636 (100 mg/kg) induces complete tumor stasis in an OCI-Ly19 diffuse large B cell lymphoma (DLBCL) mouse xenograft model and complete tumor regression in a Z-138 ibrutinib-resistant mantle cell lymphoma mouse xenograft model. It also increases DHO levels and reduces pyrimidine levels in Z-138 and JeKo-1 lymphoma mouse xenograft models.Formal Name: 1-methyl-5-(2'-methyl[1,1'-biphenyl]-4-yl)-1H-benzotriazole-7-carboxylic acid. CAS Number: 1623416-31-8. Molecular Formula: C21H17N3O2. Formula Weight: 343.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble, Water: slightly soluble. lambdamax: 259 nm. SMILES: O=C(C1=CC(C2=CC=C(C3=C(C)C=CC=C3)C=C2)=CC4=C1N(C)N=N4)O. InChi Code: InChI=1S/C21H17N3O2/c1-13-5-3-4-6-17(13)15-9-7-14(8-10-15)16-11-18(21(25)26)20-19(12-16)22-23-24(20)2/h3-12H,1-2H3,(H,25,26). InChi Key: GSBZRCGZLMBSNY-UHFFFAOYSA-N.