SMILES string
O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(C4CCCC4)[C@@H]5CC)=NC=C3N(C)C5=O)C(OC)=C2
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Application
BI 2536 may be used in targeting polo-like kinase 1 (PLK1) in cancer therapy; and studying its role in neuroblastoma.
Biochem/physiol Actions
BI 2536 is an ATP-competitive, potent and selective polo-like kinase 1 (Plk1) inhibitor (Plk1/2/3 IC50 = 0.83/3.5/9.0 nM; [ATP] = 7.5 µM) that induces mitotic arrest and apoptosis in human cancer cultures (EC50 <100 nM among 32 different cancer lines) and suppresses human cancer xenografts tumor growth in nude mice in vivo (50-60 mg/kg i.v. twice weekly on two consecutive days; HCT116 and NCI-H460).
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Péter Lénárt et al.
Current biology : CB, 17(4), 304-315 (2007-02-13)
The mitotic kinases, Cdk1, Aurora A/B, and Polo-like kinase 1 (Plk1) have been characterized extensively to further understanding of mitotic mechanisms and as potential targets for cancer therapy. Cdk1 and Aurora kinase studies have been facilitated by small-molecule inhibitors, but
Martin Steegmaier et al.
Current biology : CB, 17(4), 316-322 (2007-02-13)
Fine-mapping of the cell-division cycle, notably the identification of mitotic kinase signaling pathways, provides novel opportunities for cancer-drug discovery. As a key regulator of multiple steps during mitotic progression across eukaryotic species, the serine/threonine-specific Polo-like kinase 1 (Plk1) is highly
Mark Petronczki et al.
Developmental cell, 12(5), 713-725 (2007-05-10)
Cytokinesis of animal cells requires ingression of the actomyosin-based contractile ring between segregated sister genomes. Localization of the RhoGEF Ect2 to the central spindle at anaphase promotes local activation of the RhoA GTPase, which induces assembly and ingression of the
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