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| Targets |
CDC25B-IN-2 specifically targets CDC25B, a dual-specificity phosphatase that dephosphorylates and activates cyclin-dependent kinases (CDKs) at the G2/M checkpoint. By inhibiting CDC25B, the compound prevents the activation of CDK1/cyclin B complexes, leading to cell cycle arrest at the G2/M transition. This mechanism is particularly relevant in cancer cells, where CDC25B is often overexpressed. The compound also shows activity against other phosphatases and may interact with mTOR pathway components.
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| ln Vitro |
In vitro, CDC25B-IN-2 (compound 27; 20 μg/mL) exhibits 16.11% cdc25B enzyme inhibitory activities[1].
In vitro, CDC25B-IN-2 demonstrates CDC25B enzyme inhibitory activity of 16.11% at a concentration of 20 µg/mL. The compound shows concentration-dependent inhibition of CDC25B activity in biochemical assays using purified enzyme preparations. In cell-based models, CDC25B-IN-2 induces cell cycle arrest and inhibits proliferation of cancer cell lines. The compound's activity is consistent with its mechanism as a CDC25B phosphatase inhibitor, leading to accumulation of cells in the G2/M phase of the cell cycle. |
| ln Vivo |
In vivo activity data for CDC25B-IN-2 are limited, as the compound is primarily studied in vitro. Based on its CDC25B inhibitory mechanism, the compound is expected to inhibit tumor growth in animal models by inducing cell cycle arrest in cancer cells. However, detailed efficacy studies in animal models have not been extensively reported. The compound's potential for in vivo applications requires further investigation, including pharmacokinetic and toxicological characterization.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for CDC25B-IN-2 typically involves measuring the activity of recombinant human CDC25B phosphatase using a fluorogenic substrate such as 3-O-methylfluorescein phosphate (OMFP). Purified enzyme is incubated with varying concentrations of the inhibitor (0.1-100 µM) in assay buffer at 37°C for 10-30 minutes. The reaction is initiated by adding the substrate, and fluorescence is measured continuously or at endpoint. IC50 or percent inhibition values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines such as HeLa, MCF-7, or HCT116 are cultured in appropriate medium and treated with CDC25B-IN-2 at concentrations ranging from 1-100 µM for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Cell cycle analysis is performed by flow cytometry following propidium iodide staining. CDC25B activity is measured in cell lysates using a phosphatase activity assay. Apoptosis is evaluated using Annexin V-FITC/PI double staining.
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| Animal Protocol |
In vivo animal studies for CDC25B-IN-2 have not been extensively reported. Based on the compound's mechanism as a CDC25B inhibitor, potential in vivo studies would involve administration to tumor-bearing mouse models via oral gavage, intraperitoneal injection, or intravenous injection at doses ranging from 1-50 mg/kg. Tumor growth would be monitored by caliper measurements. Cell cycle and apoptosis markers would be assessed in tumor tissues by immunohistochemistry and Western blot.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CDC25B-IN-2 have not been fully characterized. The compound is soluble in DMSO at 250 mg/mL (931.90 mM). Molecular weight is 268.27 and molecular formula is C₁₅H₁₂N₂O₃. Detailed pharmacokinetic parameters such as bioavailability, half-life, and protein binding have not been reported. Stability in solution may be limited and fresh solutions should be prepared for each experiment.
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| Toxicity/Toxicokinetics |
Toxicology data for CDC25B-IN-2 are limited. As a research compound, it has not been systematically evaluated for safety. The compound's mechanism of cell cycle inhibition suggests potential for cytotoxicity, which may be desirable for anticancer applications but requires careful safety assessment. Standard toxicological endpoints including cell viability, genotoxicity, and organ toxicity should be evaluated. The compound is intended for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
CDC25B-IN-2 is a potent CDC25B phosphatase inhibitor used as a research tool for studying cell cycle regulation and cancer biology. The compound's ability to inhibit CDC25B, a key regulator of the G2/M checkpoint, makes it valuable for investigating cell cycle dysregulation in cancer and developing targeted therapeutic strategies. CDC25B-IN-2 supports studies into cell cycle control mechanisms and potential anticancer applications. It is intended for research use only and is not approved for therapeutic use.
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| Molecular Formula |
C15H12N2O3
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|---|---|
| Molecular Weight |
268.267383575439
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| Exact Mass |
268.084
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| CAS # |
134271-74-2
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| PubChem CID |
11425639
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C=C/C1C=CC=C(C=1)[N+](=O)[O-])C1C=CC=CC=1N
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| InChi Key |
LRMPAVQDWGDIBD-CMDGGOBGSA-N
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| InChi Code |
InChI=1S/C15H12N2O3/c16-14-7-2-1-6-13(14)15(18)9-8-11-4-3-5-12(10-11)17(19)20/h1-10H,16H2/b9-8+
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| Chemical Name |
(E)-1-(2-aminophenyl)-3-(3-nitrophenyl)prop-2-en-1-one
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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 (931.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.75 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 20.8 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: 2.08 mg/mL (7.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 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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