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WP1874 is a mesylate salt derivative of WP1244, developed as a highly potent, water-soluble, unique DNA-binding small molecule anticancer agent. The molecule comprises DNA intercalating and minor-groove-binding modules, conferring high cytotoxicity (IC50 in the low nanomolar range) against brain cancer cell lines including ependymoma, glioblastoma multiforme (GBM), and medulloblastoma, while demonstrating minimal cytotoxicity toward normal cells. WP1874 is notable for its high central nervous system (CNS) penetration and 100–200 times greater potency than doxorubicin in preclinical models. Its improved solubility supports intravenous formulations. Preclinical data suggest potential safety and high CNS accumulation, with ongoing development for treatment of CNS malignancies and consideration for other brain-involved metastases such as pancreatic, ovarian, and lymphoma cancers[1][4].
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