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CCT 137690

CCT 137690
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Purity:99.82%
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CCT 137690

Catalog No. T2611Cas No. 1095382-05-0
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).
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Pack SizePriceAvailabilityQuantity
2 mg$51In Stock
5 mg$72In Stock
10 mg$93In Stock
25 mg$181In Stock
50 mg$328In Stock
100 mg$510In Stock
1 mL x 10 mM (in DMSO)$87In Stock
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Product Introduction

Bioactivity
Description
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).
Targets&IC50
Aurora C:19 nM, Aurora A:15 nM, Aurora B:25 nM
In vitro
In transgenic mouse models of neuroblastoma, CCT137690 significantly inhibits tumor cell growth. Similarly, in SW620 colon carcinoma xenograft models, oral administration of CCT137690 can suppress cell growth.
In vivo
CCT137690 acts as an inhibitor of the hERG ion channels (IC50=3.0 μM) and effectively suppresses cell growth across various human tumor cell lines from different organs. It exhibits potent inhibitory effects on SW620 colon cancer cells (GI50=0.3 μM) and A2780 ovarian cancer cells (GI50=0.14 μM).
Kinase Assay
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.
Cell Research
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)
AliasCCT137690
Chemical Properties
Molecular Weight551.48
FormulaC26H31BrN8O
Cas No.1095382-05-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55.2 mg/mL (100 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8133 mL9.0665 mL18.1330 mL90.6651 mL
5 mM0.3627 mL1.8133 mL3.6266 mL18.1330 mL
10 mM0.1813 mL0.9067 mL1.8133 mL9.0665 mL
20 mM0.0907 mL0.4533 mL0.9067 mL4.5333 mL
50 mM0.0363 mL0.1813 mL0.3627 mL1.8133 mL
100 mM0.0181 mL0.0907 mL0.1813 mL0.9067 mL

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