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PEP07 is an orally bioavailable, brain-penetrant small molecule inhibitor of checkpoint kinase 1 (Chk1), developed for its potential antineoplastic and chemosensitization activities. By selectively binding to Chk1, PEP07 inhibits its activity and disrupts the repair of damaged DNA in cancer cells, thereby enhancing the cytotoxic effects of DNA-damaging agents. It is being investigated primarily for relapsed/refractory acute myeloid leukemia (AML), mantle cell lymphoma (MCL), metastatic solid tumors, and non-small cell lung cancer. The drug is currently in Phase 1 clinical trials[1][2][3][4][5][7].
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