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Cat. No. Name Size Price Add Cart
KI2010SCH-5271235 mg$686.4
SCH-52712310 mg$943.8
SCH-52712350 mg$2745.6
SCH-527123200 mg$6292

Chemical Characteristic

Product NameSCH-527123
SynonymsN/A
CAS No.473727-83-2
Molecular Weight 397.42
FormulaC21H23N3O5
Chemical Name3-((3-((dimethylamino)carbonyl)-2-hydroxyphenyl)amino)-4-(((r)-1-(5-methylfuran-2-yl)propyl)amino)cyclobut-3-ene-1,2-dione
SmilesC(=O)(c1c(c(ccc1)NC1=C(C(=O)C1=O)NC(CC)c1oc(cc1)C)O)N(C)C
Chemical Structure

Biological activities

SCH-527123 is a novel antagonist of both CXCR1 and CXCR2 with IC50s of 36 and 2.6 nM, respectively.[1] It binds with high affinity to the CXCR2 receptors of mouse, rat, and cynomolgus monkey with Kd values of 0.20, 0.20, and 0.08 nM, respectively. SCH-527123 also potently inhibits CXCR2-mediated chemotaxis with an IC50 of approximately 3-6 nM, and weakly inhibits cynomolgus CXCR1-mediated chemotaxis with an IC50 of approximately 1 μM. In vivo, oral administration of SCH-527123 prevents pulmonary neutrophilia (ED50 = 1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, oral administration of SCH-527123 also suppresses the pulmonary neutrophilia (ED50 = 1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50 ≤0.1 mg/kg) induced by intratracheal (i.t.) LPS.[2] Moreover, SCH-527123 treatment significantly decreases tumor growth and microvessel density in colorectal cancer xenografts models in vivo.[3]

Protocols

In vivo: Prior to use, SCH-527123 is dissolved in 10 ml of 20% HPβCD by sonication.[4]

References

[1] Dwyer MP, et al. Discovery of 3,4-diaminocyclobut-3-ene-1,2-dione-based CXCR2 receptor antagonists for the treatment of inflammatory disorders. Curr Top Med Chem. 2010, 10(13): 1339-1350.
[2] Chapman RW, et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther. 2007, 322(2): 486-493.
[3] Ning Y, et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. Mol Cancer Ther. 2012, 11(6): 1353-1364.
[4] Varney ML, et al. Small molecule antagonists for CXCR2 and CXCR1 inhibit human colon cancer liver metastases. Cancer Lett. 2011, 300(2): 180-188.

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