WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406162
CAS#: 942947-93-5
Description: CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. 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. CCT129202 may be a candidate as MDR reversal agent for antineoplastic combination therapy and merits further clinical investigation.
Hodoodo Cat#: H406162
Name: CCT129202
CAS#: 942947-93-5
Chemical Formula: C23H25ClN8OS
Exact Mass: 496.16
Molecular Weight: 497.016
Elemental Analysis: C, 55.58; H, 5.07; Cl, 7.13; N, 22.55; O, 3.22; S, 6.45
Synonym: CCT129202; CCT-129202; CCT 129202.
IUPAC/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
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)
SMILES Code: O=C(NC1=NC=CS1)CN2CCN(C3=C4C(NC(C5=CC=C(N(C)C)C=C5)=N4)=NC=C3Cl)CC2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 497.02 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Cheng C, Liu ZG, Zhang H, Xie JD, Chen XG, Zhao XQ, Wang F, Liang YJ, Chen LK, Singh S, Chen JJ, Talele TT, Chen ZS, Zhong FT, Fu LW. Enhancing Chemosensitivity in ABCB1- and ABCG2-Overexpressing Cells and Cancer Stem-like Cells by An Aurora Kinase Inhibitor CCT129202. Mol Pharm. 2012 Jun 13. [Epub ahead of print] PubMed PMID: 22632055.
2: 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 Dec;6(12 Pt 1):3147-57. PubMed PMID: 18089709.