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.
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- CAS No.: 29115-34-2
- 화학식: C12H11BrO3
- 분자량:283.12
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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.
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Cell Line:Human cancer cell lines (A549, K562, MCF-7, HCT116 p53+/+, HepG2, U87MG, CCRF-CEM, CEM/ADR5000)
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Concentration:0.001-100 μmol/L
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Incubation Time:72 h
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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.
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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]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; daily; 16 days
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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
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CAS No. 29115-34-2
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분자량 283.12
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화학식 C12H11BrO3
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SMILES
O=C(OCC)C=1OC=2C=CC=CC2C1CBr
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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)
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