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DN015089 is an orally bioavailable small molecule inhibitor of Son of Sevenless homolog 1 (SOS1), developed by Shanghai Dino Pharmaceutical Technology. SOS1 is a guanine nucleotide exchange factor (GEF) that plays a critical role in the activation of KRAS by facilitating the exchange of GDP for GTP. By binding to SOS1, DN015089 prevents the formation of the active SOS1-KRAS complex, thereby inhibiting downstream oncogenic signaling through the MAPK/ERK pathway. This mechanism is particularly relevant in cancers driven by KRAS mutations, where SOS1 acts as a key regulator of RAS activity. DN015089 is currently being evaluated in Phase 1 clinical trials for the treatment of advanced or metastatic solid tumors, including colorectal cancer, lung cancer, and other malignancies harboring RAS pathway alterations.
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