BD103

BD103 is a novel, small-molecule negative allosteric modulator (NAM) of the C-X-C chemokine receptor type 3 (CXCR3). Developed by the Tschammer lab at Friedrich Alexander University Erlangen-Nuremberg, BD103 exhibits probe-dependent inhibition of CXCR3 signaling, demonstrating greater efficacy in blocking CXCL11-mediated versus CXCL10-mediated G-protein coupled receptor (GPCR) signaling. In preclinical models of breast cancer, BD103 has been shown to target cancer stem cells (CSCs) by inhibiting tumorsphere formation and reversing ligand-mediated induction of the aldehyde dehydrogenase-positive (ALDH1+) cell fraction. Furthermore, BD103 effectively inhibits tumor cell colonization and metastasis in the lung, a protective effect associated with the reversal of CXCR3 ligand-mediated activation of downstream STAT3, ERK1/2, CREB, and NOTCH1 signaling pathways.

Other names

N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-4-(4-fluorobutoxy)-N-((1-methylpiperidin-4-yl)methyl)butanamideN-1-{[3-(4-Ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]ethyl}-4-(4-fluorobutoxy)-N-[(1-methylpiperidin-4-yl)methyl]butanamide