MCC1019
MCC1019 is a selective PLK1 PBD inhibitor with an IC50 of 16.4 μmol/L. MCC1019 inactivates the AKT signaling pathway in cancer cells, and induces Apoptosis, Necroptosis and Autophagy. MCC1019 exhibits anticancer activity against lung cancer and prostate cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 29115-34-2
- Formule: C12H11BrO3
- Masse moléculaire:283.12
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
PLK1 PBD 16.4 μM (IC50) |
MCC1019 potently and selectively inhibits PLK1 PBD, with an IC50 of 16.4 μM in cell-free biochemical assays[1].
MCC1019 inactivates the AKT signaling pathway, inhibits cell replication, and induces mitotic catastrophe in lung adenocarcinoma A549 cells[1].
MCC1019 binds to PLK1 (Kd = 12.77 μmol/L) and PLK1 PBD (Kd = 18.9 μmol/L)[2].
MCC1019 (10-40 μmol/L; 24 h) induces concentration-dependent G2/M cell cycle arrest in human lung adenocarcinoma A549 cells[2].
MCC1019 (40 μmol/L; 48 h) induces autophagy in the lung adenocarcinoma cell line A549[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human cancer cell lines (A549, K562, MCF-7, HCT116 p53+/+, HepG2, U87MG, CCRF-CEM, CEM/ADR5000)
-
Concentration:0.001-100 μmol/L
-
Incubation Time:72 h
-
Result:Exhibited cytotoxicity across all tested cell lines, with IC50 values of 23.7 ± 3.7 μmol/L (A549), 2.2 ± 0.09 μmol/L (K562), 25.4 ± 4.08 μmol/L (MCF-7), 18.7 ± 2.8 μmol/L (HCT116 p53+/+), 21.3 ± 3.6 μmol/L (HepG2), 22.7 ± 6.06 μmol/L (U87MG), 1.6 ± 0.24 μmol/L (CCRF-CEM), and 1.3 ± 0.4 μmol/L (CEM/ADR5000).
MCC1019 (40 mg/kg; i.p.; daily; 14 days) induces 61.5% prostate tumor growth inhibition with no significant body weight changes in syngeneic murine prostate cancer models[2].
MCC1019 (100-200 mg/kg; p.o.; daily; 7 days) results in 100% survival and no significant body weight loss in healthy C57BL/6 mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 mice (male and female, 8 weeks old, body weight 25 ± 5 g, syngeneic model via subcutaneous injection of LLC-1 lung cancer cells)[2]
-
Dosage:20 mg/kg; 40 mg/kg
-
Administration:i.p.; daily; 16 days
-
Result:Induced 51.1% tumor growth inhibition and reduced average lung metastatic burden area to 0.1% (from 4.1% in vehicle controls).
Induced 68.1% tumor growth inhibition and reduced average lung metastatic burden area to 2.1%.
Did not cause significant changes in body weight or weights of heart, liver, lung, or kidney (only a minor change in spleen weight was observed).
Downregulated BUBR1 expression in LLC-1 tumors.
Chemical Information
-
CAS No. 29115-34-2
-
Masse moléculaire 283.12
-
Formule C12H11BrO3
-
SMILES
O=C(OCC)C=1OC=2C=CC=CC2C1CBr
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Farhat J, et al. Structure-Activity Relationship of Benzofuran Derivatives with Potential Anticancer Activity. Cancers (Basel). 2022;14(9):2196. Published 2022 Apr 28. [Content Brief]
[2]. Abdelfatah S, et al. MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate. Acta Pharm Sin B. 2019;9(5):1021-1034. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MCC1019 Related Classifications
HY-W162436 Related Classifications
Powered by Bioz