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MCC1019

Chemical Structure : MCC1019

CAS No.: 29115-34-2

MCC1019 (MCC 1019)

Catalog No.: PC-20477Not For Human Use, Lab Use Only.

MCC1019 is a selective inhibitor of PLK1, targets PLK1 Polo box domain (PBD) with binding IC50 of 16.4 uM, 2.75-fold over PLK2-PBD (IC50=44.1 uM) and > 6-fold higher specificity over PLK3 PBD (IC50 >100 uM).

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Biological Activity

MCC1019 is a selective inhibitor of PLK1, targets PLK1 Polo box domain (PBD) with binding IC50 of 16.4 uM, 2.75-fold over PLK2-PBD (IC50=44.1 uM) and > 6-fold higher specificity over PLK3 PBD (IC50 >100 uM).
MCC1019 exerted profound cytotoxicity across a panel of cancer cell lines, hematologic malignancies (CCRF-CEM, K562 and CEM/ADR5000) were more sensitive to MCC1019 (IC50s <2 uM).
MCC1019 inhibit downstream effector proteins of PLK1 (BUBR1, p-AKT, p-FOXO1 and HIF-1α), induced M phase cell cycle arrest, and apoptosis and necroptosis.
MCC1019 (20 and 40 mg/kg) significantly inhibited tumor growth in LLC-1 lung tumor bearing mice and RM-1 prostate tumor bearing mice models.

Physicochemical Properties

M.Wt 283.12
Formula C12H11BrO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

ethyl 3-(bromomethyl)benzofuran-2-carboxylate

References

1. Abdelfatah S, et al. Acta Pharm Sin B. 2019 Sep;9(5):1021-1034.

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