Chemical Structure : MSC778
CAS No.:
3098173-17-9
MSC778
(MSC-778)
Catalog No.: PC-25526Not For Human Use, Lab Use Only.
MSC778 (MSC-778) is a potent, selective, and orally bioavailable inhibitor of Flap endonuclease 1 (FEN1) with IC50 of 3.0 nM and SPR KD of 2.9 nM, >65-fold selective over closely related RAD2 family members EXO1, GEN1 and XPG.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MSC778 (MSC-778) is a potent, selective, and orally bioavailable inhibitor of Flap endonuclease 1 (FEN1) with IC50 of 3.0 nM and SPR KD of 2.9 nM, >65-fold selective over closely related RAD2 family members EXO1, GEN1 and XPG.
MSC778 displays potent cell target engagement of FEN1 in NanoBRET assays with EC50 of 31 nM.
MSC778 demonstrates a BRCA2-selective phenotype, preferentially killing BRCA2 KO DLD-1 colorectal cancer cells, with a 10-fold margin over WT DLD-1.
MSC778 displays excellent selectivity against all members of an in-house panel of the broader nuclease superfamily, with MRE11 being the next closest in activity (>1000-fold selectivity).
MSC778 potentiates the activity of PARPi niraparib in vivo to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft.
Physicochemical Properties
|
M.Wt
|
441.87
|
|
Formula
|
C22H20ClN3O5
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
(S)-2-((S)-1-(7-Chloronaphthalen-2-yl)ethoxy)-4-hydroxy-7,8,10a,11-tetrahydro-10H-pyridazino[1′,6′:4,5]pyrazino[2,1-c][1,4]oxazine-3,5-dione
|
References
1. Mann SE, et al. J Med Chem. 2025 Sep 17. doi: 10.1021/acs.jmedchem.5c01526.
Contact Us
sales@probechem.com
