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.
