BN82002

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Chemical Structure| 396073-89-5 同义名 : -
CAS号 : 396073-89-5
货号 : A1151806
分子式 : C19H25N3O4
纯度 : 98%
分子量 : 359.42
MDL号 : MFCD08276983
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(403.43 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 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. BN82002, a novel CDC25 inhibitor, inhibits in vitro the activity of CDC25C phosphatase in a concentration dose manner with an IC50 of 5.4 μM. All of the examined human tumor cell lines were sensitive to BN82002 in a concentration-dependent manner in the low micromolar range. The most sensitive was the pancreatic cancer cell line MIA PaCa-2 with an IC50 of 7.2 μM. Treatment with BN82002 at 50 μM and 100 μM for 1 hour induced an accumulation of the tyrosine 15-phosphorylated form of CDK1. The inhibition of CDK-1 dephosphorylation suggests that BN82002 efficiently down-regulates the activity of the CDC25C phosphatase toward CDK1 in cultured MIA PaCa-2 cells. In a human osteosarcoma cell line U2OS treated with 50 μM BN82002, the activity of CDC25B was inhibited by ∼60%. Collectively, these results indicate that treatment with BN82002 inhibits CDC25 phosphatase activity in cultured cells. After 24 h of treatment by 50 μM BN82002 in HeLa cells, a concentration that fully inhibits cell proliferation, the cell cycle distribution was only modestly affected with a slight decrease in S phase and an increase in cells containing both a G1 and a G2 DNA content, suggesting that the cells treated with BN82002 were arrested at various stages of the cell cycle. In athymic mice xenografted with the human pancreatic cell MIA PaCa-2, BN82002 stabilized tumor growth during the once daily × 10 days at 15 mg/kg treatment and induced a delay in the once weekly × 3 weeks at 40 mg/kg schedule[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.82mL

5.56mL

2.78mL
参考文献

[1]Brezak MC, Quaranta M, Mondésert O, et al. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004;64(9):3320-3325