Preferred Label : Lartesertib;
NCIt synonyms : Ataxia Telangiectasia Mutated Kinase Inhibitor M4076; ATM Kinase Inhibitor M4076;
NCIt definition : 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.;
UNII : KL7B6D38VC;
CAS number : 2020089-41-0;
Molecule name : M-4076; M 4076;
NCI Metathesaurus CUI : CL1662749;
Origin ID : C180326;
UMLS CUI : C5854872;
Semantic type(s)
- concept_is_in_subset
- has_target
