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Purity: ≥98%
CCT137690 is a novel, potent, highly selective and orally bioavailable inhibitor of Aurora kinase A/B/C with potential antitumor activity. It inhibits Aurora A/B/C with IC50s of 15 nM, 25 nM and 19 nM respectively and shows no/little effect on hERG potassium ion-channel. CCT137690 shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy.
| ln Vitro |
In a variety of human tumor cell lines, such as the SW620 colon carcinoma (GI50=0.30 μM) and the A2780 ovarian cancer cell line (GI50=0.14 μM), CCT 137690 exhibits antiproliferative activity. In vitro phosphorylation of histone H3 is inhibited by CCT 137690. The hERG ion-channel is moderately inhibited by CCT 137690 (IC50=3.0 μM)[1]. HeLa and HCT116 cells are effectively inhibited by CCT137690-mediated phosphorylation of histone H3 and TACC3, which are substrates for Aurora B and Aurora A, respectively. Multipolar spindle formation, chromosome misalignment, polyploidy, and apoptosis are all brought on by the inhibitor's continuous exposure to tumor cells[2].
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| ln Vivo |
With no discernible toxicity, CCT 137690 reduces the growth of the SW620 xenografts[1]. In a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is susceptible to spontaneous neuroblastoma development, CCT 137690 effectively reduces tumor growth[2].
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| References |
[1]. Bavetsias V, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28.
[2]. Faisal A, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23 |
| Molecular Formula |
C26H31BRN8O
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| Molecular Weight |
551.48
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| CAS # |
1095382-05-0
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| Related CAS # |
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| SMILES |
CN1CCN(C2=CC=C(C3=NC4=C(N5CCN(CC6=NOC(C)=C6)CC5)C(Br)=CN=C4N3)C=C2)CC1
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| InChi Key |
GFLQCBTXTRCREJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31BrN8O/c1-18-15-20(31-36-18)17-33-9-13-35(14-10-33)24-22(27)16-28-26-23(24)29-25(30-26)19-3-5-21(6-4-19)34-11-7-32(2)8-12-34/h3-6,15-16H,7-14,17H2,1-2H3,(H,28,29,30)
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| Chemical Name |
6-Bromo-7-[4-[(5-methyl-3-isoxazolyl)methyl]-1-piperazinyl]-2-[4-(4-methyl-1-piperazinyl)phenyl]-3H-imidazo[4,5-b]pyridine
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| Synonyms |
CCT-137690; CCT 137690; CCT137690
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80:~30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8133 mL | 9.0665 mL | 18.1330 mL | |
| 5 mM | 0.3627 mL | 1.8133 mL | 3.6266 mL | |
| 10 mM | 0.1813 mL | 0.9067 mL | 1.8133 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
CCT137690 reduces MYCN levels and GSK3β phosphorylation in the KELLY neuroblastoma cell line. Mol Cancer Ther. 2011 Nov; 10(11): 2115–2123. |
CCT137690 inhibits growth of MYCN-induced neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov; 10(11): 2115–2123. |
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