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
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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]. |
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| Related Catalog | |
| 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 |
| 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 |