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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.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | 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. |
| In vitro | MSC778 selectively eradicates BRCA2 knockout DLD-1 cells over a seven-day period, with an apparent EC50 of 210 nM. The protein binding-adjusted free EC50 (EC50,ub) is 11 nM. |
| In vivo | MSC778 (100 mg/kg, oral gavage, twice daily for 28 days) enhanced the tumor-suppressing activity of Niraparib in a mouse colorectal cancer xenograft model. |
| Molecular Weight | 441.87 |
| Formula | C22H20ClN3O5 |
| Cas No. | 3098173-17-9 |
| Smiles | O=C1C=2N(C[C@@]3(N1CCOC3)[H])N=C(O[C@@H](C)C4=CC5=C(C=C4)C=CC(Cl)=C5)C(=O)C2O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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