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CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. CCT129202, a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. This compound showed high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines. Importantly, CCT129202 increased the inhibitory effect of vincristine and paclitaxel on ABCB1 overexpressing KBv200 cell xenografts in nude mice and human esophageal cancer tissue overexpressing ABCB1 ex vivo, respectively. Furthermore, the ATPase activity of ABCB1 was inhibited by CCT129202. Homology modeling predicted the binding conformation of CCT129202 within the large hydrophobic cavity of ABCB1. On the other hand, CCT129202 neither apparently altered the expression levels of ABCB1 and ABCG2 nor inhibited the activity of Aurora kinases in MDR cells under the concentration of reversal MDR. In conclusion, CCT129202 significantly reversed ABCB1- and ABCG2-mediated MDR in vitro, in vivo and ex vivo by inhibiting the function of their transporters and enhanced the eradication of cancer stem-like cells by chemotherapeutic agents.
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Source | Mol Pharm (2013). Figure 2. CCT-129202 |
| Method | MTT assay | |
| Cell Lines | SP and NSP cells of A549 | |
| Concentrations | 0.25 μM | |
| Incubation Time | 24 h | |
| Results | CCT129202 significantly abolished the drug-resistant ability of SP cells to doxorubicin but did not alter IC50 value of doxorubicin in NSP cells |
| Cell Experiment | |
|---|---|
| Cell lines | Colo205, SW620, HT29, KW12, Hela, A2780, OVCAR8, MDA-MB-157, MV4-11 and HCT-116 cells line |
| Preparation method | Cell Viability Assay. The effects of CCT129202 on cell proliferation were analyzed with the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay according to the manufacturer's instructions. Cells were plated in 96-well plates at 2,500 per well and were treated with a range of 0 to 50 μmol/L of CCT129202 for 72 h. The absorbance was measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter. |
| Concentrations | 0~10 μ M |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | human HCT116 colon carcinoma xenografts |
| Formulation | 10% DMSO, 5% Tween 20, and 85% sterile saline at 0.1 mL/10 g |
| Dosages | 5 mg/kg |
| Administration | i.p. |
| Molecular Weight | 497.02 |
| Formula | C23H25ClN8OS |
| CAS Number | 942947-93-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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