MSC778 is a potent and orally bioavailable inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of 3 nM and a KD of 2.9 nM. It demonstrates significant selectivity with 145-fold, 516-fold, and 65-fold greater inhibition over EXO1, GEN1, and XPG, respectively. MSC778 preferentially induces apoptosis in BRCA2-deficient cells and enhances the efficacy of Niraparib in tumor stasis within BRCA2 knockout DLD-1 mouse xenografts. This compound is valuable for research focused on colorectal cancer.
MSC778 is a potent and orally bioavailable inhibitor of flap endonuclease 1 (FEN1), exhibiting an IC50 of 3 nM and a KD of 2.9 nM. It demonstrates significant selectivity with 145-fold, 516-fold, and 65-fold greater inhibition over EXO1, GEN1, and XPG, respectively. MSC778 preferentially induces apoptosis in BRCA2-deficient cells and enhances the efficacy of Niraparib in tumor stasis within BRCA2 knockout DLD-1 mouse xenografts. This compound is valuable for research focused on colorectal cancer.
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