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SI306 is a small molecule competitive inhibitor of the non-receptor tyrosine kinase c-Src, belonging to the pyrazolo[3,4-d]pyrimidine class. It has demonstrated notable antitumor activity in preclinical in vitro and in vivo studies, particularly against neuroblastoma and glioblastoma models. SI306 reduces phosphorylation of focal adhesion kinase (FAK) and suppresses expression of epidermal growth factor receptor (EGFR). Due to poor aqueous solubility, several prodrugs and formulations have been developed to improve its bioavailability and pharmacokinetics, including encapsulation in pegylated stealth or antibody-targeted liposomes, and gold nanoparticle conjugates. SI306 is being evaluated as a lead compound for anticancer drug development, especially for central nervous system tumors such as glioblastoma and neuroblastoma[1][2][3][7][10].
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