Uproleselan sodium (GMI1271; GMI-1271), the sodium salt of Uproleselan, is a novel, synthetic, glycomimetic small molecule and potent E-Selectin antagonist (Kd = 0.46 uM; IC50 = 1.75 uM) with potential antineoplastic (e.g. anti-leukemic activity), anti-thrombotic, and chemopotentiating activities. It disrupts cell survival pathways, enhances chemotherapy response, improves survival in mouse xenograft and syngeneic models, and decreases chemotherapy toxicity in vivo. Upon administration, uproleselan binds to E-selectin expressed on endothelial cells and prevents their interaction with selectin-E ligand-expressing cancer cells. This may prevent tumor cell activation, migration and metastasis. GMI-1271 also interferes with the binding of selectin E-expressing vascular endothelial cells to selectin-E ligand-expressing monocytes and neutrophils, thereby disrupting their activation. Consequently, this inhibits both the activation of the coagulation cascade and thrombus formation. This agent also prevents both leukocyte activation and inflammation. E-selectin is a cell adhesion molecule involved in cell rolling, signaling and chemotaxis; it also plays a crucial role in inflammatory processes and cancer.
纯度:≥98%
CAS:1914993-95-5