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CCT-129202

Cat. No. M1691
CCT-129202 Structure
Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 510 In stock
200mg USD 1380 In stock
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Quality Control
Biological Activity

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.

Protocol
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 (Sigma) 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 (PerkinElmer).
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 497.02
Formula C23H25ClN8OS
CAS Number 942947-93-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

Enhancing Chemosensitivity in ABCB1- and ABCG2-Overexpressing Cells and Cancer Stem-like Cells by An Aurora Kinase Inhibitor CCT129202.
Cheng C, et al. Mol Pharm. 2012 Jun 13. PMID: 22632055.

Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity.
Chan F, et al. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57. PMID: 18089709.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCT-129202 supplier, Aurora Kinase, inhibitors

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