| Name | CCT 137690 |
| 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). |
| 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) |
| 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. |
| 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). |
| Storage | Powder: -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)
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| Keywords | CCT-137690 | CCT 137690 | Inhibitor | inhibit | Aurora Kinase | Apoptosis |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library |
United States
