MSC778 is a selective and orally active inhibitor of flap endonuclease 1 (FEN1), with an IC50 of 3 nM and a KD of 2.9 nM. It exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively targets BRCA2-deficient cells and enhances the tumor-stalling activity of Niraparib in BRCA2 KO DLD-1 mouse xenografts. It is applicable in colorectal cancer research.
Molekulargewicht:
441.87
CAS Nummer:
[3098173-17-9]
Formel:
C22H20ClN3O5
Target-Kategorie:
FLAP
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