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M3541 is a potent, selective, orally active ATM inhibitor with potential chemo-/radio-sensitizing and antineoplastic activities. M-3541 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, M 3541 sensitizes tumor cells to chemo- and radiotherapy. ATM, a serine/threonine protein kinase, is upregulated in a variety of cancer cell types; it is activated in response to DNA damage and plays a key role in DNA-strand repair.

M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities[1].

[1] Astrid Zimmermann, et al. A New Class of Selective ATM Inhibitors as Combination Partners of DNA Double-Strand Break Inducing Cancer Therapies. Mol Cancer Ther. 2022 Jun 1;21(6):859-870. DOI:10.1158/1535-7163.MCT-21-0934