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BAPT-31 is a novel small-molecule macropinocytosis inducer (MPI) belonging to the BAPT (3-(((3-mercapto-5-(pyridin-4-yl)-4H-1,2,4-triazol-4-yl)imino)methyl)quinolin-2-ol) chemical series. It is being developed as a therapeutic adjuvant to enhance the intracellular delivery of both small-molecule and macromolecular drugs in aggressive and multidrug-resistant (MDR) cancers, including colorectal cancer (CRC) and triple-negative breast cancer (TNBC). BAPT-31 functions by stimulating macropinocytosis, a non-selective endocytic pathway that allows cells to engulf large volumes of extracellular fluid and its contents. By inducing this process, BAPT-31 increases the uptake and bioavailability of co-administered agents such as albumin, dextran, and chemotherapeutics like doxorubicin and paclitaxel, potentially overcoming the efflux-mediated resistance common in advanced tumors. Preclinical studies have demonstrated that BAPT-31 significantly enhances the cytotoxicity of these anticancer drugs in various cancer cell lines by facilitating their entry into the cytoplasm.
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