NCIt definition : A small molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic
sensitizing activity. Adavosertib selectively targets and inhibits WEE1, a tyrosine
kinase that phosphorylates cyclin-dependent kinase 1 (CDK1, CDC2) to inactivate the
CDC2/cyclin B complex. Inhibition of WEE1 activity prevents the phosphorylation of
CDC2 and impairs the G2 DNA damage checkpoint. This may lead to apoptosis upon treatment
with DNA damaging chemotherapeutic agents. Unlike normal cells, most p53 deficient
or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the
G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged
cells. Annulment of the G2 checkpoint may therefore make p53 deficient tumor cells
more vulnerable to antineoplastic agents and enhance their cytotoxic effect.;
UNII : K2T6HJX3I3;
InChIKey : BKWJAKQVGHWELA-UHFFFAOYSA-N;
CAS number : 955365-80-7; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 955365-80-7
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