Synonym
BN-82002; BN 82002; BN82002; CDC25 Phosphatase Inhibitor I; PTP Inhibitor XX;
IUPAC/Chemical Name
Phenol, 4-(dimethylamino)-2-methoxy-6-((methyl(2-(4-nitrophenyl)ethyl)amino)methyl)-
InChi Key
GOKYHQGRIIXMNE-UHFFFAOYSA-N
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
SMILES Code
OC1=C(CN(C)CCC2=CC=C([N+]([O-])=O)C=C2)C=C(N(C)C)C=C1OC
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
CDC25 dual-specificity phosphatases are essential regulators that dephosphorylate and activate cyclin-dependent kinase/cyclin complexes at key transitions of the cell cycle. CDC25 activity is currently considered to be an interesting target for the development of new antiproliferative agents
Biological target:
BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family.
In vitro activity:
BN82002 dose-dependently down-regulated mRNA levels of nitric oxide synthase, tumor necrosis factor-α, and cyclooxygenase-2. The nuclear translocation of nuclear factor (NF)-κB (p65 and p50) was also blocked by BN82002 in RAW265.7 cells stimulated by LPS.
Reference: Biochem Pharmacol. 2019 Jun;164:216-227. https://pubmed.ncbi.nlm.nih.gov/30980807/
In vivo activity:
On the basis of the in vitro results, the activity of BN82002 was evaluated in athymic mice xenografted with the human pancreatic cell MIA PaCa-2. BN82002 stabilized tumor growth during the once daily × 10 treatment and induced a delay in the once weekly × 3 schedule.
Reference: Cancer Res. 2004 May 1;64(9):3320-5. https://pubmed.ncbi.nlm.nih.gov/15126376/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
150.0 |
417.33 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
359.43
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Kim HG, Yang WS, Hong YH, Kweon DH, Lee J, Kim S, Cho JY. Anti-inflammatory functions of the CDC25 phosphatase inhibitor BN82002 via targeting AKT2. Biochem Pharmacol. 2019 Jun;164:216-227. doi: 10.1016/j.bcp.2019.04.007. Epub 2019 Apr 10. PMID: 30980807.
2. Brezak MC, Quaranta M, Mondésert O, Galcera MO, Lavergne O, Alby F, Cazales M, Baldin V, Thurieau C, Harnett J, Lanco C, Kasprzyk PG, Prevost GP, Ducommun B. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5. doi: 10.1158/0008-5472.can-03-3984. PMID: 15126376.
3. Brezak MC, Quaranta M, Mondésert O, Galcera MO, Lavergne O, Alby F, Cazales M, Baldin V, Thurieau C, Harnett J, Lanco C, Kasprzyk PG, Prevost GP, Ducommun B. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5. doi: 10.1158/0008-5472.can-03-3984. PMID: 15126376.
In vitro protocol:
1. Kim HG, Yang WS, Hong YH, Kweon DH, Lee J, Kim S, Cho JY. Anti-inflammatory functions of the CDC25 phosphatase inhibitor BN82002 via targeting AKT2. Biochem Pharmacol. 2019 Jun;164:216-227. doi: 10.1016/j.bcp.2019.04.007. Epub 2019 Apr 10. PMID: 30980807.
2. Brezak MC, Quaranta M, Mondésert O, Galcera MO, Lavergne O, Alby F, Cazales M, Baldin V, Thurieau C, Harnett J, Lanco C, Kasprzyk PG, Prevost GP, Ducommun B. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5. doi: 10.1158/0008-5472.can-03-3984. PMID: 15126376.
In vivo protocol:
1. Brezak MC, Quaranta M, Mondésert O, Galcera MO, Lavergne O, Alby F, Cazales M, Baldin V, Thurieau C, Harnett J, Lanco C, Kasprzyk PG, Prevost GP, Ducommun B. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5. doi: 10.1158/0008-5472.can-03-3984. PMID: 15126376.
1: Brenner AK, Reikvam H, Rye KP, Hagen KM, Lavecchia A, Bruserud Ø. CDC25 Inhibition in Acute Myeloid Leukemia-A Study of Patient Heterogeneity and the Effects of Different Inhibitors. Molecules. 2017 Mar 11;22(3). pii: E446. doi: 10.3390/molecules22030446. PubMed PMID: 28287460; PubMed Central PMCID: PMC6155411.
2: Yamashita Y, Kasugai I, Sato M, Tanuma N, Sato I, Nomura M, Yamashita K, Sonoda Y, Kumabe T, Tominaga T, Katakura R, Shima H. CDC25A mRNA levels significantly correlate with Ki-67 expression in human glioma samples. J Neurooncol. 2010 Oct;100(1):43-9. doi: 10.1007/s11060-010-0147-3. Epub 2010 Mar 10. PubMed PMID: 20217459.
3: Contour-Galcéra MO, Lavergne O, Brezak MC, Ducommun B, Prévost G. Synthesis of small molecule CDC25 phosphatases inhibitors. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5809-12. PubMed PMID: 15501045.
4: Brezak MC, Quaranta M, Mondésert O, Galcera MO, Lavergne O, Alby F, Cazales M, Baldin V, Thurieau C, Harnett J, Lanco C, Kasprzyk PG, Prevost GP, Ducommun B. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5. PubMed PMID: 15126376.
