2. Immunology/Inflammation
  3. FLAP
  4. 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.

For research use only. We do not sell to patients.

MSC778

MSC778 Chemical Structure

CAS No. : 3098173-17-9

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MSC778 Related Antibodies

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Description

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[1].

In Vitro

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.

MSC778 Related Antibodies
Parmacokinetics[1]
Species Dose Route Indicator value
Dog 0.2 mg/kg i.v. Cmax 1240 ng/mL
Dog 16 mg/kg p.o. Cmax 6000 ng/mL
Mice 0.2 mg/kg i.v. Cmax 2490 ng/mL
Mice 10 mg/kg p.o. Cmax 6030 ng/mL
Mice 30 mg/kg p.o. Cmax 30500 ng/mL
Rat 0.2 mg/kg i.v. Cmax 1950 ng/mL
Rat 10 mg/kg p.o. Cmax 5860 ng/mL
Dog 0.2 mg/kg i.v. AUC 2520 ng·h/mL
Dog 16 mg/kg p.o. AUC 43200 ng·h/mL
Mice 0.2 mg/kg i.v. AUC 8510 ng·h/mL
Mice 10 mg/kg p.o. AUC 56900 ng·h/mL
Mice 30 mg/kg p.o. AUC 229536 ng·h/mL
Rat 0.2 mg/kg i.v. AUC 2240 ng·h/mL
Rat 10 mg/kg p.o. AUC 27400 ng·h/mL
Dog 16 mg/kg p.o. F 21 %
Mice 10 mg/kg p.o. F 16 %
Mice 30 mg/kg p.o. F 16 %
Rat 10 mg/kg p.o. F 15 %
In Vivo

MSC778 (100 mg/kg, i.g., twice daily for 28 days) potentiates the activity of Niraparib to induce tumor stasis in a mouse colorectal cancer xenograft model[1].

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.
Molecular Weight

441.86

Formula

C22H20ClN3O5
CAS No.
SMILES

ClC1=CC2=CC([C@@H](OC3=NN(C[C@@H](COCC4)N4C5=O)C5=C(O)C3=O)C)=CC=C2C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MSC778 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MSC7783098173-17-9MSC 778MSC-778FLAP5-lipoxygenase-activating protein5-LO activating proteinFragment-Based Drug DiscoveryBRCA2 KO DLD-1 CellsMouse Xenograft ModelSPRPK/ADME ProfileInhibitorinhibitorinhibit

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