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lartesertib

An orally bioavailable ATP-competitive inhibitor of ataxia telangiectasia mutated kinase (ATM), with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, lartesertib targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, by preventing DNA damage repair, M4076 sensitizes tumor cells to chemo- and radiotherapy and increases their anti-tumor activity. ATM, a serine/threonine protein kinase upregulated in a variety of cancer cell types, is activated in response to DNA damage and plays a key role in DNA-strand repair.
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Synonym:ataxia telangiectasia mutated kinase inhibitor M4076
ATM kinase inhibitor M4076
Code name:M 4076
M-4076
M4076
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