CCT129202

Alias: CCT-129202; CCT 129202; CCT129202.
Cat No.:V0359 Purity: ≥98%
CCT129202 (CCT-129202), animidazopyridine compound,is a potent andATP-competitive pan-Aurora inhibitor with potential antitumor activity.
CCT129202 Chemical Structure CAS No.: 942947-93-5
Product category: Aurora Kinase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

CCT129202 (CCT-129202), an imidazopyridine compound, is a potent and ATP-competitive pan-Aurora inhibitor with potential antitumor activity. It inhibits Aurora A, Aurora B and Aurora C with IC50s of 0.042 μM, 0.198 μM and 0.227 μM, respectively. CCT129202 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Apoptosis results from the increase of z4N-containing human tumor cells brought on by CCT129202. It is discovered that CCT129202 induces apoptosis, with GI50 values ranging from 0.08 to 1.7 μM. Human tumor cells treated with CCT120202 exhibit spindle abnormalities, abrogation of nocodazole-induced mitotic arrest, and a delay in mitosis. H2F-DependentTK1Down-regulation, Rb Hypophosphorylation, and p21Up-regulation are all caused by CCT129202[1].
ln Vivo
CCT129202 is administered intraperitoneally (i.p.) to nude mice to suppress the growth of HCT116 xenografts. CCT129202 induces the cyclin-dependent kinase inhibitor p21. Thymidine kinase 1 transcription was reduced as a result of Rb hypophosphorylation and E2F suppression brought on by CCT129202's up-regulation of p21 in HCT116 cells[1].
Animal Protocol
Dissolved in 10% DMSO, 5% Tween 20 in saline; 100 mg/kg; i.p. injection
HCT116 colon carcinoma is established in female NCr athymic mice.
References
[1]. Chan F, et al. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H25CLN8OS
Molecular Weight
497.02
CAS #
942947-93-5
Related CAS #
942947-93-5
SMILES
O=C(NC1=NC=CS1)CN2CCN(C3=C4C(NC(C5=CC=C(N(C)C)C=C5)=N4)=NC=C3Cl)CC2
InChi Key
QYKHWEFPFAGNEV-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H25ClN8OS/c1-30(2)16-5-3-15(4-6-16)21-28-19-20(17(24)13-26-22(19)29-21)32-10-8-31(9-11-32)14-18(33)27-23-25-7-12-34-23/h3-7,12-13H,8-11,14H2,1-2H3,(H,25,27,33)(H,26,28,29)
Chemical Name
2-(4-(6-chloro-2-(4-(dimethylamino)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)-N-(thiazol-2-yl)acetamide
Synonyms
CCT-129202; CCT 129202; CCT129202.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 3 mg/mL (6.0 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0120 mL 10.0600 mL 20.1199 mL
5 mM 0.4024 mL 2.0120 mL 4.0240 mL
10 mM 0.2012 mL 1.0060 mL 2.0120 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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