3H-Pyrazolo[3,4-d]pyrimidin-3-one, 6-[(2',3'-dihydro-2'-methylspiro[cyclopropane-1,4'(1'H)-isoquinolin]-7'-yl)amino]-1,2-dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-2-(2-propen-1-yl)-

Biological Activity

WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities[1]. WEE1-IN-3 (example 1) inhibits cancer cell growth with IC50 values of 100-1000 nM and <100 nM for SW480 cells and H23 cells, respectively[1].WEE1 kinase plays a role in the G2-M cell-cycle checkpoint arrest for ?Να repair before mitotic entry. Normal cells repair damaged DNA during GI arrest. Cancer cells often have a deficient G i-S checkpoint and depend on a functional G2-M checkpoint for DNA repair. WEE1 is overexpressed in various cancer types[1].

References

[1]. Peter Qinhua HUANG, et al. 1, 2 - dihydro- 3h- pyrazolo [3, 4 - d] pyrimidin -3 - one analogs. WO2019028008A1.