CCT129202 |
| رقم الكتالوجGC11310 |
An Aurora kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 942947-93-5
Sample solution is provided at 25 µL, 10mM.
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CCT129202, a derivative of the piperazinyl imidazo[4,5-b] pyridine scaffold, is a novel and potent inhibitor of Aurora kinase that ATP-competitively inhibits Aurora A, Aurora B and Aurora C with values of 50% inhibition concentration IC50 of 0.042, 0.198 and 0.227 μmol/L respectively. CCT129202 exhibits anti-cancer activity against multiple human tumor cell lines through inhibiting proliferation, inducing apoptosis and delaying mitosis, abrogation of nocodazole-induced mitotic arrest and spindle defects. Recent study results have shown that CCT129202 inhibits the growth of HCT116 xenografts in nude mice and induces the production of a cyclin-dependent kinase inhibitor, p21, in HCT116 cells consequently leading to Rb hypophosphorylation.
Reference
[1].Chan F, Sun C, Perumal M, Nguyen QD, Bavetsias V, McDonald E, Martins V, Wilsher NE, Raynaud FI, Valenti M, Eccles S, Te Poele R, Workman P, Aboagye EO, Linardopoulos S. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther. 2007; 6(12 Pt1): 3147-3157.
| Cell experiment [1]: | |
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Cell lines |
MV4-11 cell lines, MDA-MB-157 cell lines |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
24 h |
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Applications |
CCT129202 inhibited proliferation in multiple cultures of human tumor cell lines with half-maximal growth inhibition (GI50) values ranging from 0.08 μM for MV4-11 to 1.7 μM for MDA-MB-157. Treatment with CCT129202 (0.7 μM) caused the accumulation of HCT116 cells with ≥4N DNA content, leading to apoptosis in a time dependent manner. Application of CCT129202 in HCT116 cells decreased histone H3 phosphorylation and increased p53 protein stabilization. CCT129202 induced up-regulation of p21 in HCT116, HT29 and Hela cells in a p53 dependent and independent manner. CCT129202 decreased phosphorylation of the Rb protein and activity of E2F in a concentration-dependent manner. |
| Animal experiment [1]: | |
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Animal models |
Female NCr athymic mice human HCT116 colon carcinoma xenografts |
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Dosage form |
Intraperitoneal injection, 100 mg/kg |
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Application |
Administration of CCT129202 at 100 mg/kg in athymic mice bearing s.c. HCT116 colon cancer xenografts causes ~50% reduction of histone H3 phosphorylation after 30 minutes of treatment, and significantly inhibited tumor growth by 57.7% compared to control mice after a period of 9 days of treatment. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Chan F, Sun C, Perumal M, et al. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity[J]. Molecular Cancer Therapeutics, 2007, 6(12): 3147-3157. | |
| Cas No. | 942947-93-5 | SDF | |
| Chemical Name | 2-[4-[6-chloro-2-[4-(dimethylamino)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide | ||
| Canonical SMILES | CN(C)C1=CC=C(C=C1)C2=NC3=NC=C(C(=C3N2)N4CCN(CC4)CC(=O)NC5=NC=CS5)Cl | ||
| Formula | C23H25ClN8OS | M.Wt | 497.02 |
| الذوبان | ≥ 4.97 mg/mL in DMSO with gentle warming, <1.72 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.012 mL | 10.06 mL | 20.1199 mL |
| 5 mM | 0.4024 mL | 2.012 mL | 4.024 mL |
| 10 mM | 0.2012 mL | 1.006 mL | 2.012 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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