SCH 527123

SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1, IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells). It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation. SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively). It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.Formal Name: 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-benzamide. CAS Number: 473727-83-2. Synonyms: MK-7123. Molecular Formula: C21H23N3O5. Formula Weight: 397.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Methanol: slightly soluble. lambdamax: 215, 296, 347 nm. SMILES: OC1=C(C(N(C)C)=O)C=CC=C1NC(C2=O)=C(N[C@@H](C3=CC=C(C)O3)CC)C2=O. InChi Code: InChI=1S/C21H23N3O5/c1-5-13(15-10-9-11(2)29-15)22-16-17(20(27)19(16)26)23-14-8-6-7-12(18(14)25)21(28)24(3)4/h6-10,13,22-23,25H,5H2,1-4H3/t13-/m1/s1. InChi Key: RXIUEIPPLAFSDF-CYBMUJFWSA-N.