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CCT 137690
- Moderately soluble in DMSO
- MF: C26H31BrN8O
- MW: 551.48
Description
CCT 137690 is a potent and orally bioavailable Aurora kinase inhibitor with reported IC50 values of 15 nM, 25 nM and 19 nM for Aurora A, Aurora B and Aurora C, respectively.
Aurora kinases control mitotic entry, centrosome function, spindle assembly and chromosome segregation. CCT 137690 is useful for investigating mitotic checkpoint failure, polyploidy and antiproliferative responses in oncology models.
Key Features
- Pan-Aurora kinase inhibitor
- IC50: 15 nM for Aurora A, 25 nM for Aurora B and 19 nM for Aurora C
- Orally bioavailable mitotic kinase research compound
- Induces pathway effects linked to cell-cycle disruption
Applications
- Aurora kinase pharmacology
- Mitosis and spindle checkpoint studies
- Cancer cell-cycle and antiproliferative assays
- Kinase selectivity and mitotic biomarker profiling
More Information
| Parent CAS No. | 1095382-05-0 |
|---|---|
| Chemical Name | 3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole |
| SMILES | C1(Br)C(N2CCN(CC3C=C(C)ON=3)CC2)=C2N=C(C3C=CC(N4CCN(C)CC4)=CC=3)NC2=NC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C26H31BrN8O/c1-18-15-20(31-36-18)17-33-9-13-35(14-10-33)24-22(27)16-28-26-23(24)29-25(30-26)19-3-5-21(6-4-19)34-11-7-32(2)8-12-34/h3-6,15-16H,7-14,17H2,1-2H3,(H,28,29,30) |
| InChiKey | GFLQCBTXTRCREJ-UHFFFAOYSA-N |
| CID | 25154041 |
| Short Description | Aurora inhibitor |
References
- V Bavetsias et al. 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. 2010, 53(14), 5213-5228.
- A Faisal et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol. Cancer Ther. 2011, 10(11), 2115-2123.
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