SF1126

SF1126 is an investigational small molecule drug that acts as a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), with additional activity against DNA-dependent protein kinase (DNA-PK) and bromodomain-containing protein 4 (BRD4)[1][2][3]. It is a water-soluble prodrug composed of the pan-PI3K/mTOR inhibitor LY294002 conjugated to an RGD-containing peptide, which targets integrins expressed on tumor vasculature to enhance tumor-specific delivery[1][2][3][5]. Upon administration, it is hydrolyzed in vivo to release the active drug. The mechanism involves inhibition of all class IA PI3K isoforms as well as mTOR and DNA-PK, disrupting key signaling pathways involved in tumor cell proliferation, survival, angiogenesis, and resistance to chemotherapy[2][3]. Developed originally by Semafore Pharmaceuticals and later by SignalRx Pharmaceuticals, SF1126 has shown antitumor and antiangiogenic activity in preclinical models. It has been evaluated in phase I/II clinical trials for advanced solid tumors and B-cell malignancies such as chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), head and neck cancer, among others[4][7].

Other names

SF-1126 INNER SALTSF1126 INNER SALTSF 1126 INNER SALT