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CGP 57380
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CGP 57380图片
CAS NO:522629-08-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)244.23
FormulaC11H9FN6
CAS No.522629-08-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 48 mg/mL (196.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 10 mg/mL
SynonymsCGP57380; CGP-57380; CGP 57380
实验参考方法
In Vitro

In vitro activity: CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). CGP57380 prevents the serial replating function of BC progenitors.


Kinase Assay: CGP 57380 is potent inhibitor of MNK1 with IC50 value of 2.2 μM.


Cell Assay: In 293 cells, CGP 57380 (10 μM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 μM. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way. In mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. In bone marrow-derived macrophages, CGP 57380 significantly inhibited the production of proinflammatory cytokines monocyte chemoattractant protein-1, TNF and IL-6.

In VivoCGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs.
Animal modelIn mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. Also, CGP 57380 inhibited eIF4E phosphorylation.
Formulation & Dosage
References

Mol Cell Biol. 2001 Aug;21(16):5500-11; Circ Res. 2003 Dec 12;93(12):1218-24; Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307.