MedKoo product information:

MSX-122

Description of MSX-122: MSX-122 is an orally bioavailable inhibitor of CXCR4 with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the GPCR (G protein-coupled receptor) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; it is also a co-receptor for HIV entry into T cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   Metastatix Inc.

MSX-122 is a potent inhibitor of the chemokine receptor CXCR4, which is activated by stromal derived factor-1 (SDF-1). The interaction between SDF-1 and CXCR4 has been shown to promote chemotaxis and angiogenesis in multiple cancer cell types. In preclinical studies, MSX-122 has displayed a favorable pharmacodynamic and safety profile while inhibiting the function of CXCR4, thus affecting downstream cellular events. [source: http://www.gabio.org/pr_details.aspx?subid=121] .

1. Guo, Hongyan; Kim, Choung U.; Lee, Ill Young; Mitchell, Michael L.; Rhodes, Gerry; Son, Jong Chan; Xu, Lianhong. Preparation of pyrimidindiones as HIV reverse transcriptase inhibitors. PCT Int. Appl. (2009), 466pp. CODEN: PIXXD2 WO 2009005674 A2 20090108 CAN 150:144497 AN 2009:20492 CAPLUS

2. He, Gong-Xin; Kim, Choung U.; Mitchell, Michael L.; Xu, Lianhong. Preparation of pyrimidinediones as HIV reverse transcriptase inhibitors. PCT Int. Appl. (2009), 145pp. CODEN: PIXXD2 WO 2009005693 A1 20090108 CAN 150:121677 AN 2009:20491 CAPLUS.

3. Weiqiang Zhan's Ph.D dissertation, title: Part I: Design, Synthesis and Biological Evaluation of C6-C8 Bridged Epothilone Analogs, Part II: Discovery of Small Molecule CXCR4 Antagonists,  Emory University, this dissertation can be download from Emory University:  https://etd.library.emory.edu/file/view/pid/emory.../zhan_dissertation.pdf.