Drug intelligence / Profile preview

si306

Development stage
Preclinical
Lead developer
Lead Discovery Siena
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

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].

Other names
SI306SI-306SI 306pyrazolo[3,4-d]pyrimidine derivative SI306
02

Targets

SRC (Proto-oncogene tyrosine-protein kinase Src)

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