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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3098173-17-9
- Fòrmula: C22H20ClN3O5
- Peso molecular:441.86
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
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.
-
Animal Model:BRCA2 KO DLD-1 cells xenograft model established in Balb/c nude, female mice[1]
-
Dosage:100 mg/kg with or without Niraparib
-
Administration:Oral gavage (i.g.), twice daily for 28 days
-
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
-
No. CAS 3098173-17-9
-
Peso molecular 441.86
-
Fòrmula C22H20ClN3O5
-
SMILES
ClC1=CC2=CC([C@@H](OC3=NN(C[C@@H](COCC4)N4C5=O)C5=C(O)C3=O)C)=CC=C2C=C1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MSC778 Related Classifications
HY-177512 Related Classifications
Powered by Bioz