CCT129202

SKU: orb1685696

Description

CCT129202 is a potent, ATP-competitive pan-Aurora kinase inhibitor, demonstrating highest activity against Aurora A. It serves as a valuable chemical probe for studying mitotic progression, cell cycle dysregulation, and oncology research in both cellular and biochemical assays.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 942947-93-5
• MW: 497.02
• Purity: 98.14% (May vary between batches)
• Formula: C₂₃H₂₅ClN₈OS
• SMILES: CN(C)c1ccc(cc1)-c1nc2c(N3CCN(CC(=O)Nc4nccs4)CC3)c(Cl)cnc2[nH]1
• Target: Aurora Kinase
• Solubility: DMSO:4.98 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  Aurora B:198 nM|Aurora A:42 nM|Aurora C:227 nM
• In Vivo:
  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 inhibits tumor growth by 57.7% compared to control mice after a period of 9 days of treatment.
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• In Vitro:
  CCT129202 is an ATP-competitive inhibitor of recombinant Aurora A kinase with a Ki of 49.8 nM. CCT129202 at 1 μM shows high selectivity for Aurora A and Aurora B with 92% and 60% inhibition, respectively. It inhibits FGFR3 slightly by 27%, and is not active against CRAF. CCT129202 inhibits 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. The effects are in association with increased expression levels of Aurora A and Aurora B leading to aberrant mitosis. Treatment with CCT129202 (0.7 μM) causes the accumulation of HCT116 cells with ≥4N DNA content, leading to apoptosis in a time dependent manner. Application of CCT129202 in HCT116 cells causes decreased histone H3 phosphorylation and increased p53 protein stabilization, which are consistent with the inhibition of Aurora B and Aurora A, respectively. CCT129202 induces up-regulation of p21 in HCT116, HT29 and Hela cells in a p53 dependent and independent manner, which leads to decreased phosphorylation of the Rb protein and activity of E2F in a concentration-dependent manner.
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• Cell Research:
  Cells are treated with a range of 0 to 50 uM of CCT129202 for 72 hours. Cell proliferation is analyzed with the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The absorbance is measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AuroraKinase, Aurora Kinase, Aurora C, Aurora B, Aurora A, CCT 129202, CCT129202, CCT-129202, Inhibitor, inhibit

Compound Identifiers

PubChem CID

16202152