Name: CGP-53716
Rating: 5 (10 reviews)

有库存

sdf 文件

结构编辑

类似物检索

HIT ID:HIT212036536
Cas No:152459-94-4
常用名:CGP-53716
IUPAC:N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide
IUPAC:N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide
InChI key:UOEJSOXEHKCNAE-UHFFFAOYSA-N

分子式:C23H19N5O
分子量:381.439
氢键供体数 (HBD):2
氢键受体数 (HBA):5
LogP:4.5891566
SMILES:Cc1ccc(NC(=O)c2ccccc2)cc1Nc1nccc(n1)-c1cccnc1
SMILES:Cc1ccc(NC(=O)c2ccccc2)cc1Nc1nccc(n1)-c1cccnc1

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 formationin 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 injuryin 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].

市场产品/服务共显示3个结果

供应商
TargetMolSC
规格
货期
5日内发货
纯度
-
¥ 2,298.00
1
供应商
EnamineSC
规格
货期
4-6周
纯度
-
¥ 512.00
1
供应商
BIONET-Key OrganicsBB
规格
货期
4-6周
纯度
-
¥ 8,149.00
1

寻找合适的化合物库

您无法确定哪种化合物库最适合您的项目？或者您需要定制解决方案？Anymole随时为您提供帮助。

电话：400820-0310

合作：info@screeningcompound.com

技术支持：tech@screeningcompound.com

客服：service@screeningcompound.com

正在加载 ~