I-1000233

I-1000233 is a brain-permeable, allosteric small molecule inhibitor of SHP2 (Src homology phosphotyrosyl phosphatase 2), developed by IRBM Science Park SpA. It is designed to selectively and potently inhibit SHP2, a key regulator in the RAS-MAPK signaling pathway that drives tumor growth and survival. The compound’s unique ability to cross the blood-brain barrier positions it as a promising candidate for treating central nervous system (CNS) malignancies such as brain metastases and primary brain cancers—areas with significant unmet medical need due to limited therapeutic options. Preclinical studies have demonstrated strong antitumor efficacy and favorable pharmacokinetics. Additionally, its mechanism may help overcome resistance to EGFR inhibitors in various cancer types[1][2][3][6].