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251356-45-3

中文名称 化合物 T16947
英文名称 SU 16f
CAS 251356-45-3
分子式 C24H22N2O3
分子量 386.44
MOL 文件 251356-45-3.mol
更新日期 2024/09/25 10:08:25
251356-45-3 结构式 251356-45-3 结构式

基本信息

中文别名
化合物SU16F
化合物 T16947
英文别名
SU 16f
PDGFR Tyrosine Kinase Inhibitor VII - CAS 251356-45-3 - Calbiochem
(Z)-3-(2,4-Dimethyl-5-((2-oxo-6-phenylindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
5-[1,2-Dihydro-2-oxo-6-phenyl-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-propanoicacid
1H-Pyrrole-3-propanoic acid, 5-[(1,2-dihydro-2-oxo-6-phenyl-3H-indol-3-ylidene)methyl]-2,4-dimethyl-

物理化学性质

沸点661.7±55.0 °C(Predicted)
密度1.292±0.06 g/cm3(Predicted)
储存条件Store at RT
溶解度Soluble to 100 mM in DMSO
酸度系数(pKa)4?+-.0.10(Predicted)
形态暗橙色固体
颜色Yellow to orange

常见问题列表

生物活性
SU16f 是有效的,选择性 PDGFRβ 抑制剂,对 PDGFRβ,PDGFR1,PDGFR2 的 IC50 分别为 10 nM,140 nM,2.29 μM。SU16f 抑制 PDGFRβ 受体从而可以阻断胃癌来源的间充质干细胞 (GC-MSC) 条件培养基在胃癌细胞增殖和迁移中的促进作用。
靶点

PDGFRβ

10 nM (IC 50 )

PDGFR2

140 nM (IC 50 )

PDGFR1

2.29 μM (IC 50 )

体外研究

SU16f (20 μM; for 8 hours) pretreatment inhibits the promoting role of GC-MSC-CM in SGC-7901 cell proliferation.
SU16f (20 μM; for 8 hours) significantly abolishes PDGFRβ activation in SGC-7901 by GC-MSC-CM. SU16f pretreatment results in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA. SU16f pretreatment leads to downregulation of p-AKT, Bcl-xl, and Bcl-2 levels and upregulation of Bax expression in SGC-7901 cells by GC-MSC-CM .

Cell Proliferation Assay

Cell Line: SGC-7901 cells in GC-MSC/SGC-7901 co-culture system
Concentration: 20 μM
Incubation Time: 8 hours
Result: Inhibited the promoting role of GC-MSC-CM in SGC-7901 cell proliferation.

Western Blot Analysis

Cell Line: SGC-7901 cells
Concentration: 20 μM
Incubation Time: 8 hours
Result: Significantly abolished PDGFRβ activation in SGC-7901 by GC-MSC-CM, and resulted in the upregulation of E-cadherin and downregulation of N-cadherin, Vimentin, and α-SMA.
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