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MSC778

MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer[1].

Product Specifications

CAS Number

[3098173-17-9]

UNSPSC

12352005

Target

FLAP

Related Pathways

Immunology/Inflammation

Field of Research

Cancer

Smiles

ClC1=CC2=CC([C@@H](OC3=NN(C[C@@H](COCC4)N4C5=O)C5=C(O)C3=O)C)=CC=C2C=C1

Molecular Formula

C22H20ClN3O5

Molecular Weight

441.86

References & Citations

[1]Mann SE, et al. Fragment-Based Discovery and Structure-Led Optimization of MSC778, the First Potent, Selective, and Orally Bioavailable FEN1 Inhibitor. J Med Chem. 2025 Sep 17.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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