| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
BN-82002 primarily targets the CDC25 phosphatase family, which includes CDC25A, CDC25B2, CDC25B3, CDC25C, and CDC25C-cat. The IC50 values for inhibition of these isoforms are 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. CDC25 phosphatases are key regulators of the cell cycle, responsible for dephosphorylating and activating cyclin-dependent kinases (CDKs). By inhibiting CDC25 phosphatases, BN-82002 prevents the activation of CDKs, leading to cell cycle arrest and inhibition of tumor cell proliferation. The compound does not compete with ATP for binding, as it targets a phosphatase rather than a kinase.
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| ln Vitro |
BN82002's impact on cell proliferation was assessed in vitro using a variety of human tumor cell lines. The control was menadione, which has been shown to impede the growth of cells. In the low micromolar range, all tested cell lines exhibited concentration-dependent sensitivity to BN82002 and menadione. With an IC50 of 7.2 μM, the pancreatic cancer cell line MIA PaCa-2 is the most sensitive, while the colon cancer cell line HT-29 has an IC50 of 32.6 μM, making it the least sensitive. The activity range is strikingly similar to that of menadione (5–15 μM). Additionally, it was demonstrated that cells treated with BN82002 were arrested because 50 μM of the compound completely inhibited cell proliferation, with only a moderate impact on cell cycle distribution. This included a slight decrease in S phase and an increase in cells with G1 and G2 DNA content. during different phases of the cell cycle [1].
In vitro, BN-82002 inhibits the proliferation of various human tumor cell lines. It impairs the proliferation of tumorally bioavailable cell lines and increases cyclin-dependent kinase 1 (CDK1) inhibitory tyrosine phosphorylation. In synchronized HeLa cells, BN-82002 treatment leads to cell cycle arrest. The compound's irreversible inhibition of CDC25 phosphatases results in sustained cell cycle inhibition, making it a valuable tool for studying the role of CDC25 in cancer cell proliferation and for exploring the therapeutic potential of CDC25 inhibitors. |
| ln Vivo |
Specific in vivo activity data for BN-82002 is not detailed in the provided search results. As an anti-tumor compound, its efficacy would be evaluated in animal models of cancer, such as mouse xenograft models. The compound would be administered via intraperitoneal or oral routes, and tumor growth inhibition would be assessed. Its ability to increase CDK1 tyrosine phosphorylation and induce cell cycle arrest in tumor tissues would be evaluated as pharmacodynamic markers. Further studies are needed to characterize its in vivo efficacy and safety profile.
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| Enzyme Assay |
The in vitro activity of BN-82002 is assessed using cell-free phosphatase activity assays. Recombinant CDC25 phosphatases are incubated with a fluorogenic or chromogenic phosphatase substrate in the presence of varying concentrations of BN-82002. The dephosphorylation of the substrate is measured spectrophotometrically or fluorometrically. The IC50 is determined from dose-response curves. For selectivity profiling, the compound is tested against a panel of other phosphatases to assess its specificity. The irreversible nature of the inhibition can be confirmed by dialysis or dilution experiments.
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| Cell Assay |
For cellular assays, various cancer cell lines are cultured in appropriate media and treated with various concentrations of BN-82002 (typically 0.1-100 µM) for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle analysis is performed by flow cytometry using propidium iodide staining. The phosphorylation status of CDK1 (Tyr15) is analyzed by Western blotting using phospho-specific antibodies. The expression of cell cycle regulators (e.g., cyclins, CDKs) is also evaluated by Western blotting or qPCR. Apoptosis is assessed by measuring caspase-3/7 activity or by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
In vivo, BN-82002 would be administered to mice bearing human tumor xenografts. The compound is formulated in a suitable vehicle (e.g., 5% DMSO, 40% PEG300, 5% Tween-80, and 50% ddH2O) and administered at various doses (typically 10-100 mg/kg) via intraperitoneal or oral administration. Tumor growth is monitored by measuring tumor volume. At the end of the study, tumors are excised and analyzed for CDK1 phosphorylation, cell cycle markers, and apoptosis. Pharmacodynamic studies involve collecting tumor tissue at various time points to assess target engagement and pathway modulation.
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| ADME/Pharmacokinetics |
BN-82002 has a molecular weight of 359.42 g/mol and a molecular formula of C19H25N3O4. It has a purity of ≥95%. The compound is soluble in DMSO and should be stored as a powder at -20°C. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's cell-permeable nature allows it to reach intracellular targets in vitro and in vivo.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BN-82002 is not available in the provided search results. As a CDC25 phosphatase inhibitor, it may affect normal cell cycle progression in rapidly dividing tissues, potentially leading to myelosuppression or gastrointestinal effects. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile.
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| References | |
| Additional Infomation |
BN-82002 is a research compound that has been developed as a potent and selective CDC25 phosphatase inhibitor. It is used as a tool to study cell cycle regulation and the role of CDC25 phosphatases in cancer. The compound's irreversible inhibition of CDC25 phosphatases makes it a valuable probe for investigating the therapeutic potential of CDC25 inhibitors in oncology. BN-82002 is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C19H25N3O4
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| Molecular Weight |
359.426
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| Exact Mass |
359.185
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| CAS # |
396073-89-5
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| Related CAS # |
BN82002 hydrochloride;1049740-43-3
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| PubChem CID |
9798923
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.572
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GOKYHQGRIIXMNE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25N3O4/c1-20(2)17-11-15(19(23)18(12-17)26-4)13-21(3)10-9-14-5-7-16(8-6-14)22(24)25/h5-8,11-12,23H,9-10,13H2,1-4H3
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| Chemical Name |
Phenol, 4-(dimethylamino)-2-methoxy-6-((methyl(2-(4-nitrophenyl)ethyl)amino)methyl)-
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| Synonyms |
BN-82002 BN 82002 BN82002 CDC25 Phosphatase Inhibitor I PTP Inhibitor XX
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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 : ≥ 150 mg/mL (~417.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.96 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 25.0 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: ≥ 2.5 mg/mL (6.96 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 25.0 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 | 2.7822 mL | 13.9109 mL | 27.8218 mL | |
| 5 mM | 0.5564 mL | 2.7822 mL | 5.5644 mL | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7822 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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