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MSC778

Chemical Structure : MSC778

CAS No.: 3098173-17-9

MSC778 (MSC-778)

货号: 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 441.87
分子式 C22H20ClN3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

1. Mann SE, et al. J Med Chem. 2025 Sep 17. doi: 10.1021/acs.jmedchem.5c01526.

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