CCT137690是一种有口服活性的极光激酶抑制剂，对极光激酶A、B和C的IC50值分别为15、25 和19 nM。

CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM).

在转基因鼠成神经细胞瘤模型中,CCT137690明显抑制肿瘤细胞生长.在SW620结肠癌移植瘤模型中, 口服CCT137690能够抑制细胞生长.

对于hERG离子通道（IC50=3.0 μM）,CCT137690能够起到抑制作用。在多种人类不同器官肿瘤细胞系中, CCT137690能够有效抑制细胞生长。对于SW620结肠癌细（GI50=0.3 μM）,A2780卵巢癌细胞（GI50=0.14 μM）。

Flashplate assay for identification and evaluation of Aurora inhibitors: On this assay 384-well Basic Flashplate? as solid assay platform is used. The plates are coated overnight at 4 °C with dithiothreitol (DTT) at 100 μg/mL in PBS buffer and used after being washed twice with PBS. 5 μL of CCT137690 in 2% DMSO is added to each well followed by 15 μL master mix of kinase buffer (50 mM Tris pH 7.5, 10 mM NaCl, 2.5 mM MgCl2, 1 mM myelin basic protein (MBP), 20 μM ATP, and 0.025 μCi/μL 33P-ATP). Finally, 250 ng per well of Aurora-A enzyme is added. The plate is shaken for approximately 2 min on a flat-bed plate shaker and incubated for 2 hours at room temperature. The reaction is stopped by washing the plate twice on a 16-pin wash with 10 mM sodium pyrophosphate. The plate is then read on a TopCount-NXTTM. For the determination of the inhibitory activity against Aurora-B or Aurora-C, the same conditions are followed in the assay using Aurora-B or Aurora-C enzymes.

The effects of CCT137690 on cell proliferation are analyzed with the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells such as SW620 and A2780 are plated in 96-well plates at 2.5 × 103 per well and are treated with a range of 0 to 50 μM of CCT137690 for 72 hours. The absorbance is measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter.(Only for Reference)

1095382-05-0

C26H31BrN8O

551.493

CCT137690

DMSO:55.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years