CCT129202 Chemical Properties

Density 

1.427

storage temp. 

Store at -20°C

solubility 

DMSO : 1 mg/mL (2.01 mM; Need ultrasonic)

form 

Powder

pka

9.26±0.50(Predicted)

color 

Light yellow to yellow

InChIKey

QYKHWEFPFAGNEV-UHFFFAOYSA-N

SMILES

N1(CC(NC2=NC=CS2)=O)CCN(C2C(Cl)=CN=C3NC(C4=CC=C(N(C)C)C=C4)=NC3=2)CC1

CCT129202 Usage And Synthesis

Uses

CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.

Biological Activity

CCT129202 is an ATP-competitive pan-Aurora inhibitor with IC50s of 0.042 μM, 0.198 μM and 0.227 μM for Aurora A, Aurora B and Aurora C, respectively, and has a weaker effect on FGFR3, GSK3β, PDGFRβ, etc.

in vivo

CCT129202 at a dose of 100 mg/kg subcutaneously injected HCT116 colon xenografts in athymic mice, after 30 minutes, caused a ~50% decrease in histone H3 phosphorylation, and after 9 days of treatment, significantly inhibited tumor growth, compared with the control group , inhibited by 57.7%.

target

Aurora A

IC 50

Aurora A: 42 nM (IC₅₀); Aurora B: 198 nM (IC₅₀); Aurora C: 227 nM (IC₅₀)

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. DOI:10.1158/1535-7163.MCT-07-2156

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