Biological Activity
Potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively). Displays antiproliferative activity in a range of human tumor cell lines. Orally bioavailable.
Compound Libraries
CCT 137690 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 551.48 |
Formula | C26H31BrN8O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 1095382-05-0 |
PubChem ID | 25154041 |
InChI Key | GFLQCBTXTRCREJ-UHFFFAOYSA-N |
Smiles | CN(CC4)CCN4C(C=C3)=CC=C3C2=NC1=C(N5CCN(CC6=NOC(C)=C6)CC5)C(Br)=CN=C1N2 |
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 | 55.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 551.48. 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 | 1.81 mL | 9.07 mL | 18.13 mL |
5 mM | 0.36 mL | 1.81 mL | 3.63 mL |
10 mM | 0.18 mL | 0.91 mL | 1.81 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bavetsias et al (2010) Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J.Med.Chem. 53 5213 PMID: 20565112
Faisal et al (2011) The Aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol.Cancer Ther. 10 2115 PMID: 21885865
Keywords: CCT 137690, supplier, CCT137690, aurora, kinases, pan-aurora, inhibitors, inhibits, antiproliferative, Aurora, Kinases, Aurora, Kinases, Tocris Bioscience