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CAS No.: 152459-94-4

CGP-53716 Catalog No. CSN20482

Synonyms: CGP-53716

CGP-53716 is a selective tyrosine kinase inhibitor of PDGFR.

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技术信息

生物活性

描述The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation^[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smooth muscle cell) proliferation and migration in vitro and in neointimal formation in vivo^[3]. CGP 53716 inhibited serum-induced cell growth in RASMC (rat aortic smooth muscle cells). And it completely blocked PDGF-BB tyrosine receptor autophosphorylation in RASMC and 3T3 cells, PDGF-BB-induced phosphorylation of mitogen-activated protein kinase at 1 μM in RASMC and inhibited PDGF-BB-induced c-Fos protein expression at 1 μM in RASMC; consistent with inhibition of PDGF-BB-induced DNA synthesis. Further, CGP 53716 inhibited PDGF-BB-, bFGF- and EGF-induced DNA synthesis in a concentration-dependent manner in each cell line. And it showed a 2- to 4-fold selectivity for PDGF-BB-stimulated DNA synthesis over bFGF or EGF in RASMC or 3T3 cells^[1]. CGP 53716 inhibited dose dependently tyrosine phosphorylation of both the known PDGFRs: the PDGFR-α and PDGFR-β. After rat carotid artery ballooning injury in vivo, the migration of alpha-actin-positive cells on the luminal side of internal elastic lamina was decreased with 50 mg/kg/day of CGP 53716 from 38 ± 10 (control group) to 4 ± 2. Intima/media ratio was inhibited by 40% after 14 days in the CGP 53716-treated group (P=0.028) after rat aortic denudation^[3].
参考文献

[1] Inhibition of cell growth: effects of the tyrosine kinase inhibitor CGP 53716
[2] Buchdunger E, Zimmermann J, et al. Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class. Proc Natl Acad Sci U S A. 1995 Mar 28;92(7):2558-62.
[3] Inhibition of platelet-derived growth factor receptor tyrosine kinase inhibits vascular smooth muscle cell migration and proliferation

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6217 mL
- 13.1086 mL
- 26.2171 mL
- 5 mM
- 0.5243 mL
- 2.6217 mL
- 5.2434 mL
- 10 mM
- 0.2622 mL
- 1.3109 mL
- 2.6217 mL

技术信息

CAS号	152459-94-4	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C23H19N5O	运输	蓝冰
分子量	381.43	别名	CGP-53716

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