AR-C124910XX is a potent and selective antagonist of the CXCR4 chemokine receptor. It has been primarily investigated for its ability to modulate stem cell mobilization. By blocking the CXCR4/SDF-1 (stromal cell-derived factor-1) axis, this compound effectively disrupts the interaction that retains hematopoietic stem cells in the bone marrow niche. As a result, it promotes the release of stem cells into the peripheral bloodstream.

This property makes AR-C124910XX a candidate for use in stem cell transplantation protocols, particularly in patients who are poor mobilizers of stem cells using standard therapies like G-CSF (granulocyte colony-stimulating factor). It has shown efficacy in preclinical models and early clinical trials when used alone or in combination with G-CSF to enhance stem cell harvest for autologous or allogeneic transplants.

Additionally, due to the role of CXCR4 in cancer metastasis, inflammation, and HIV infection, AR-C124910XX has been explored in oncology for its potential to interfere with tumor cell migration and homing to metastatic sites. Its application in disrupting protective tumor microenvironments is under investigation, especially in hematologic malignancies such as multiple myeloma and acute myeloid leukemia.

The compound’s pharmacokinetic profile allows for oral administration, which offers a practical advantage over injectable mobilizing agents, supporting its development as a convenient therapeutic option.