251356-45-3

251356-45-3 structure

Name: SU 16f
Chemical Name: 3-[2,4-dimethyl-5-[(2-oxo-6-phenyl-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
CAS Number: 251356-45-3
Molecular Formula: C₂₄H₂₂N₂O₃
Molecular Weight: 386.44300
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK PDGFR
Create Date: 2017-04-06 12:22:58
Modify Date: 2024-01-07 03:07:14
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].

Name	3-[2,4-dimethyl-5-[(2-oxo-6-phenyl-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
Synonyms	su 16f

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Target	PDGFRβ:10 nM (IC50) PDGFR2:140 nM (IC50) PDGFR1:2.29 μM (IC50)
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]. 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.
References	[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.

Density	1.292±0.06 g/cm3(Predicted)
Boiling Point	661.7±55.0 ℃(Predicted)
Molecular Formula	C₂₄H₂₂N₂O₃
Molecular Weight	386.44300
Exact Mass	386.16300
PSA	82.19000
LogP	4.94640
Storage condition	2-8°C

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