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.
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- CAS. Nr.: 3098173-17-9
- Formel: C22H20ClN3O5
- Molecular Weight:441.86
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
MSC778 (7 days) selectively kills BRCA2 knockout DLD-1 cells, with an EC50 value of 210 nM (apparent value) and the free EC50 (EC50,ub) after protein binding correction is 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUC | F |
|---|---|---|---|---|---|
| Dog[1] | 0.2 mg/kg | i.v. | 1240 ng/mL | 2520 ng·h/mL | / |
| Dog[1] | 16 mg/kg | p.o. | 6000 ng/mL | 43200 ng·h/mL | 21 % |
| Mice[1] | 0.2 mg/kg | i.v. | 2490 ng/mL | 8510 ng·h/mL | / |
| Mice[1] | 10 mg/kg | p.o. | 6030 ng/mL | 56900 ng·h/mL | 16 % |
| Mice[1] | 30 mg/kg | p.o. | 30500 ng/mL | 229536 ng·h/mL | 16 % |
| Rat[1] | 0.2 mg/kg | i.v. | 1950 ng/mL | 2240 ng·h/mL | / |
| Rat[1] | 10 mg/kg | p.o. | 5860 ng/mL | 27400 ng·h/mL | 15 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BRCA2 KO DLD-1 cells xenograft model established in Balb/c nude, female mice[1]
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Dosage:100 mg/kg with or without Niraparib
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Administration:Oral gavage (i.g.), twice daily for 28 days
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Result:Observed no tumor growth inhibition (TGI) with the single-agent treatment. Achieved 93% TGI in the combined treatment group, resulting in tumor stasis. No weight loss or clinical signs of toxicity.
Chemical Information
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CAS. Nr. 3098173-17-9
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Molecular Weight 441.86
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Formel C22H20ClN3O5
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SMILES
ClC1=CC2=CC([C@@H](OC3=NN(C[C@@H](COCC4)N4C5=O)C5=C(O)C3=O)C)=CC=C2C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MSC778 Related Classifications
HY-177512 Related Classifications
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