化合物 T16947

生物活性靶点体外研究化合物 T16947 试剂级价格

化合物 T16947

CAS号:251356-45-3
英文名:SU 16f
中文名:化合物 T16947
CBNumber:CB42501833
分子式:C24H22N2O3
分子量:386.44
MOL File:251356-45-3.mol

化合物 T16947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
形态 :Dark orange solid
酸度系数(pKa) :4?+-.0.10(Predicted)
颜色 :Yellow to orange

化合物 T16947性质、用途与生产工艺

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.