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CCT129202 Aurora Kinase inhibitor

Cat.No.S1519

CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
CCT129202 Aurora Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 497.02

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Quality Control

Batch: Purity: 99.68%
99.68

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (6.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 497.02 Formula

C23H25ClN8OS

 Storage (From the date of receipt)
CAS No. 942947-93-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)C1=CC=C(C=C1)C2=NC3=NC=C(C(=C3N2)N4CCN(CC4)CC(=O)NC5=NC=CS5)Cl

Mechanism of Action

Targets/IC50/Ki
Aurora A
42 nM
Aurora B
198 nM
Aurora C
227 nM
In vitro
CCT129202 is an ATP-competitive inhibitor of recombinant Aurora A kinase with a Ki of 49.8 nM. This compound 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. This inhibitor also suppresses 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 this chemical (0.7 μM) causes the accumulation of HCT116 cells with ≥4N DNA content, leading to apoptosis in a time dependent manner. Application of this agent 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. It 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.
Kinase Assay
Inhibition of Aurora Kinases
NH2-terminal glutathione S-transferase (GST)-fusion recombinant human Aurora A (aa 118-403), Aurora B (full length), and Aurora C (full length) are expressed in baculovirus, purified, and used in the kinase inhibition assays. The in vitro kinase assays are performed in kinase buffer (50 mM Tris pH 7.5, 10 mM NaCl, 2.5 mM MgCl2 and 1 mM DTT) containing γ-32P-ATP, Aurora kinase and different concentrations of this compound. The reactions are incubated for 30 minutes at 30 °C and stopped by adding sample buffer. The reactions are separated on Novex Tris-Glycine gels and dried on a vacuum gel drier at 80 °C for 1 hour before exposure to Kodak-Biomax XR film. The concentration of this chemical that inhibits Aurora kinases by 50% is calculated representing IC50 value.
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 this compound significantly inhibits tumor growth by 57.7% compared to control mice after a period of 9 days of treatment.
References

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