Adavosertib
Wee1 kinase inhibitor / Inhibits Wee1 tyrosine kinase (IC50 = 5.2 nM) thus preventing phosphorylation of CDC2 and abrogating the G2 DNA damage checkpoint, sensitizing a variety of tumor cells to DNA damaging agents.1 Adavosertib also blocks Wee1 phosphorylation of E3 ubiquitin ligase SKP2 in human cells, ultimately preventing degradation of CDKs and further allowing cell cycle progression.2 Stimulates anti-tumor immunity and enhances sensitivity to immune checkpoint blockade by activating ERV and the dsRNA pathway.3 Potentiates sensitivity of tumors to PARP inhibitors.4
Biochemicals & reagents
955365-80-7
MK-1775; AZD1775
Hirai et al. (2009) Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents; Cancer Ther. 8 2992 Pan et al. (2021) A novel WEE1 pathway for replication stress responses; Plants 7 209 Guo et al. (2022) WEE1 inhibition induces anti-tumor immunity by activating ERV and the dsRNA pathway; Exp. Med. 219 e20210789 Seo et al. (2021) Inhibition of WEE1 Potentiates Sensitivity to PARP Inhibitor in Biliary Tract Cancer; Cancer Res. Treat. Epub ahead of print
-20°C
TARGET: Kinase -- PATHWAY: Cell cycle; DNA damage; Apoptosis inducer; DNA damage; p53 -- RESEARCH AREA: Ubiquitin/Proteasome; Cancer stem cells; Immunology; Cell death -- DISEASE AREA: Cancer