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SYH2051 is a novel, selective small molecule inhibitor of ataxia telangiectasia mutated (ATM) protein kinase, developed for the treatment of advanced solid tumors and head and neck cancer. By inhibiting ATM kinase activity, SYH2051 disrupts the repair of DNA double-strand breaks through targeted inhibition of ATM phosphorylation and its downstream signaling proteins CHK2 and KAP1. This leads to persistent DNA damage, cell cycle arrest, and inhibition of tumor cell proliferation. Preclinical studies have shown that SYH2051 has high selectivity for ATM targets with promising in vitro and in vivo antitumor activity. It is being evaluated both as monotherapy and in combination with other therapies such as radiotherapy, antibody-drug conjugates (ADCs), chemotherapy, or the anti-EGFR ADC SYS6010[4][5][2][3][6].
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