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Purity: ≥98%
BN-82002, formerly known as CDC25 Phosphatase Inhibitor I, is a cell-permeable ortho-hydroxybenzylamino compound that exhibits anti-tumor properties. BN-82002 acts as a selective and irreversible (covalent) inhibitor of CDC25 phosphatase family (IC50 = 2.4, 3.9, 6.3, 5.4, and 4.6 µM for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). BN82002 inhibits the phosphatase activity of recombinant human CDC25A, B, and C in vitro. It impairs the proliferation of tumorally bioavailable cell lines and increases cyclin-dependent kinase 1 inhibitory tyrosine phosphorylation. In synchronized HeLa cells, BN82002 delays cell cycle progression at G1-S, in S phase and at the G2-M transition.
| 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].
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| References |
[1]. Brezak MC, et al. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5.
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| Molecular Formula |
C19H25N3O4
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|---|---|
| Molecular Weight |
359.426
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| Exact Mass |
359.1845
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| CAS # |
396073-89-5
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| Related CAS # |
BN82002 hydrochloride;1049740-43-3
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| SMILES |
OC1=C(CN(C)CCC2=CC=C([N+]([O-])=O)C=C2)C=C(N(C)C)C=C1OC
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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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| 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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