Biological Activity
Potent and selective PLK inhibitor (IC50 = 3 nM). Exhibits selectivity for PLK1 over a panel of other kinases. Inhibits growth of a range of tumor cells lines in vitro and induces apoptosis in leukemia cells. Exhibits antitumor activity in mouse colorectal and nasopharyngeal cancer models in vivo.
Compound Libraries
Ro 3280 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 543.61 |
| Formula | C27H35F2N7O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1062243-51-9 |
| PubChem ID | 25015677 |
| InChI Key | DJNZZLZKAXGMMC-UHFFFAOYSA-N |
| Smiles | COC1=C(C=CC(C(NC2CCN(CC2)C)=O)=C1)NC3=NC=C4N(C(C(F)(CN(C4=N3)C5CCCC5)F)=O)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.18 | 50 | |
| ethanol | 27.18 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 543.61. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.84 mL | 9.2 mL | 18.4 mL |
| 5 mM | 0.37 mL | 1.84 mL | 3.68 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.84 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cheung et al (2013) Polo-like kinase inhibitor Ro5203280 has potent antitumor activity in nasopharyngeal carcinoma. Mol.Cancer Ther. 12 1393 PMID: 23686835
Chen et al (2012) Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg.Med.Chem.Lett. 22 1247 PMID: 22172702
Wang et al (2015) Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int.J.Mol.Sci. 16 1266 PMID: 25574601
Keywords: Ro 3280, supplier, Ro3280, Polo-like, kinases, inhibitors, inhibits, apoptosis, inducers, anticancer, PLK1, potent, selective, Polo-like, Kinase, Mitosis, Polo-like, Kinase, Tocris Bioscience
