| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
cdk2-cyclin A (IC50 = 0.41 μM);CDK1-Cyclin B (IC50 = 6.6 μM); CDK4-Cyclin D (IC50 = 5.5 μM); cdk5-p25 (IC50 = 15 μM); cdk7-cyclin H (IC50 = 3.9 μM); Aurora A (IC50 = 67 nM); Aurora B (IC50 = 35 nM)
NU6140 primarily targets CDK2-cyclin A with an IC50 of 0.41 μM. It also inhibits other Cdks including CDK1-cyclin B (IC50 = 6.6 µM), CDK4-cyclin D (IC50 = 5.5 µM), CDK5-p25 (IC50 = 15 µM), and CDK7-cyclin H (IC50 = 3.9 µM). Additionally, it effectively inhibits Aurora A (IC50 = 67 nM) and Aurora B (IC50 = 35 nM). |
|---|---|
| ln Vitro |
NU6140 has IC50 values of 6.6, 5.5, 15, and 3.9 μM for CDK1-cyclin B, CDK4-cyclin D, CDK5-p25, and CDK7-cyclin H, respectively, indicating that it is less active than other cyclins.
NU6140 causes an increase in the sub-G1 apoptotic cell population and increases the catalytic activity of capases-9 and-3[1]. In vitro, NU6140 has IC50 values of 6.6, 5.5, 15, and 3.9 μM for CDK1-cyclin B, CDK4-cyclin D, CDK5-p25, and CDK7-cyclin H, respectively. It causes an increase in the sub-G1 apoptotic cell population and increases the catalytic activity of caspases-9 and -3. The compound has been shown to cause cell cycle arrest at the G2/M phase and induce apoptosis by activating caspases and down-regulating survivin. |
| ln Vivo |
In vivo, NU6140 synergistically potentiates paclitaxel cytotoxicity and apoptotic response in HeLa and OAW42 cells. This suggests that combining NU6140 with paclitaxel may enhance the anti-tumor efficacy of the chemotherapeutic agent. While specific in vivo animal model data for NU6140 alone is limited, its ability to potentiate paclitaxel indicates potential for combination therapy in cancer treatment.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for NU6140 involve kinase activity assays using purified CDK/cyclin complexes or Aurora kinases. The compound's inhibitory activity is measured by monitoring the phosphorylation of a substrate peptide or protein in the presence of ATP. IC50 values are determined from dose-response curves. ATP-competition assays can be performed to confirm the mode of inhibition.
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| Cell Assay |
In vitro cellular assays for NU6140 are conducted in cancer cell lines such as HeLa and OAW42. Cells are treated with the compound, and cell cycle distribution is analyzed by flow cytometry to assess G2/M phase arrest. Apoptosis is evaluated by measuring sub-G1 population, caspase-9 and -3 activity, and survivin expression levels. Combination studies with paclitaxel are performed to assess synergistic cytotoxicity.
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| Animal Protocol |
In vivo animal studies for NU6140 are not extensively documented in the available literature. However, the compound's ability to potentiate paclitaxel cytotoxicity in vitro suggests that in vivo efficacy studies could be conducted in xenograft mouse models. Animals would be treated with NU6140 alone or in combination with paclitaxel, and tumor growth inhibition, apoptosis markers, and survival would be evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NU6140 indicate it is a cell-permeable compound. It has a molecular weight of 422.52, a molecular formula of C23H30N6O2, and is soluble in DMSO at 10 mg/mL. The compound is stable as a solid at 2-8°C and should be protected from light. Following reconstitution, stock solutions are stable for up to 6 months at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological information for NU6140 indicates it is classified as carcinogenic/teratogenic (D). This highlights the need for careful handling and suggests potential genotoxic or carcinogenic risks. As with other Cdk inhibitors, comprehensive toxicology studies would be required for clinical development, including assessments of mutagenicity, carcinogenicity, and reproductive toxicity.
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| References |
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| Additional Infomation |
NU6140 is a research compound primarily used as a tool for studying CDK and Aurora kinase biology in cancer research. It is also known as Cdk2 Inhibitor IV. The compound is available from various research chemical suppliers and is not approved for clinical use. Its value lies in its selectivity for CDK2 and its ability to inhibit Aurora kinases, making it useful for dissecting cell cycle regulation and apoptosis pathways.
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| Molecular Formula |
C23H30N6O2
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|---|---|
| Molecular Weight |
422.52
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| Exact Mass |
422.243
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| Elemental Analysis |
C, 65.38; H, 7.16; N, 19.89; O, 7.57
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| CAS # |
444723-13-1
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| Related CAS # |
444723-13-1
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| PubChem CID |
10202471
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| Appearance |
White to light yellow solid powder
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| LogP |
4.61
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
31
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| Complexity |
560
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)C(=O)C1=CC=C(C=C1)NC2=NC3=C(C(=N2)OCC4CCCCC4)N=CN3
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| InChi Key |
XHEQSRJCJTWWAH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30N6O2/c1-3-29(4-2)22(30)17-10-12-18(13-11-17)26-23-27-20-19(24-15-25-20)21(28-23)31-14-16-8-6-5-7-9-16/h10-13,15-16H,3-9,14H2,1-2H3,(H2,24,25,26,27,28)
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| Chemical Name |
4-[[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino]-N,N-diethylbenzamide
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| Synonyms |
NU 6140; NU-6140; NU6140
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO: ~250 mg/mL (591.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.92 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3668 mL | 11.8338 mL | 23.6675 mL | |
| 5 mM | 0.4734 mL | 2.3668 mL | 4.7335 mL | |
| 10 mM | 0.2367 mL | 1.1834 mL | 2.3668 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.
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