An Aurora kinase inhibitor
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CCT129202

Item No. 29053

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-chloro-2-[4-(dimethylamino)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]-N-2-thiazolyl-1-piperazineacetamide
CAS Number
942947-93-5
Molecular Formula
C23H25ClN8OS
Formula Weight
497.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 3 mg/ml
λmax
267, 348, 404 nm
SMILES
CN(C)C(C=C1)=CC=C1C2=NC3=NC=C(Cl)C(N4CCN(CC(NC5=NC=CS5)=O)CC4)=C3N2
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)
InChi Key
QYKHWEFPFAGNEV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $55

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    5 mg

    $215

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    10 mg

    $402

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    Product Description

    CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 μM in cell-free assays.1 It is selective for Aurora A and B over a panel of 13 kinases at 1 μM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 μM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).2 In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model.1 It also potentiates the antitumor effects of vincristine (Item No. 11764) in a KBv200 mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. Mol. Cancer Ther. 6(12 Pt 1), 3147-3157 (2007).

    2. Cheng, C., Liu, Z.-G., Zheng, H., et al. Enhancing chemosensitivity in ABCB1- and ABCG2-overexpressing cells and cancer stem-like cells by an Aurora kinase inhibitor CCT129202. Mol. Pharm. 9(7), 1971-1982 (2012).