TC-I 15

TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, ^[1][2]. IC50 & Target:IC₅₀: 0.4 μM (α2β1 to GLOGEN), 26.8 μM (α2β1 to GFOGER), 23.6 μM (α1β1 to GFOGER), 24.4 μM (α1β1 to GLOGEN), 177 μM (α11β1 to GLOGEN), 3177 μM (α11β1 to GFOGER)^[1] In Vitro:TC-I 15 (0-500 μM, 1 h) inhibits the adhesion of C₂C₁₂ cells expressing α2β1 in a dose-dependent manner, with IC₅₀ values of 26.8 μM and 0.4 μM for GFOGER and GLOGEN, respectively^[1].
TC-I 15 (0-500μM, 1 h) also inhibited α1β1, showing IC₅₀ values of 23.6 μM for GFOGER and 24.4 μM for GLOGEN^[1].
TC-I 15 (0-50μM, 1 h) inhibits the adhesion of HT1080 cells to GFOGER^[1].
TC-I 15 (0-50μM, 1 h) inhibits the uptake of EVs by LFs cells^[2]. In Vivo:TC I-15 (10 μg; intravenous injection; every other day; for three weeks) inhibits lung metastasis promoted by CAFs EVs in mice^[2].