SU16f

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SU16f  纯度: ≥99.0%

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。

SU16f

SU16f Chemical Structure

CAS No. : 251356-45-3

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生物活性

SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively[1]. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration[2].

IC50 & Target[1]

PDGFRβ

10 nM (IC50)

PDGFR2

140 nM (IC50)

PDGFR1

2.29 μM (IC50)

体外研究
(In Vitro)

SU16f (20 μM; for 8 hours) pretreatment inhibits the promoting role of GC-MSC-CM in SGC-7901 cell proliferation[1].
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 [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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.

分子量

386.44

Formula

C24H22N2O3

CAS 号

251356-45-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999 Dec 16;42(25):5120-30.

    [2]. Huang F, et al. Gastric cancer-derived MSC-secreted PDGF-DD promotes gastric cancer progression. J Cancer Res Clin Oncol. 2014 Nov;140(11):1835-48.

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