SU 16f

CAS# 251356-45-3

SU 16f

2D Structure

Catalog No. BCC7639----Order now to get a substantial discount!

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SU 16f: 5mg $115 In Stock
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3D structure

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SU 16f

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Chemical Properties of SU 16f

Cas No. 251356-45-3 SDF Download SDF
PubChem ID 5329150 Appearance Powder
Formula C24H22N2O3 M.Wt 386.44
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO
Chemical Name 3-[2,4-dimethyl-5-[(Z)-(2-oxo-6-phenyl-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
SMILES CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=C(C=C(C=C3)C4=CC=CC=C4)NC2=O
Standard InChIKey APYYTEJNOZQZNA-MOSHPQCFSA-N
Standard InChI InChI=1S/C24H22N2O3/c1-14-18(10-11-23(27)28)15(2)25-21(14)13-20-19-9-8-17(12-22(19)26-24(20)29)16-6-4-3-5-7-16/h3-9,12-13,25H,10-11H2,1-2H3,(H,26,29)(H,27,28)/b20-13-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SU 16f

DescriptionPotent and selective platelet-derived growth factor receptor β (PDGFRβ) inhibitor (IC50 = 10 nM) that displays > 14-fold, > 229-fold and > 10000-fold selectivity over VEGFR2, FGFR1 and EGFR respectively. Inhibits proliferation of HUVEC and NIH3T3 cells in vitro (IC50 = 0.11 μM).

SU 16f Dilution Calculator

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SU 16f Molarity Calculator

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Preparing Stock Solutions of SU 16f

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5877 mL 12.9386 mL 25.8772 mL 51.7545 mL 64.6931 mL
5 mM 0.5175 mL 2.5877 mL 5.1754 mL 10.3509 mL 12.9386 mL
10 mM 0.2588 mL 1.2939 mL 2.5877 mL 5.1754 mL 6.4693 mL
50 mM 0.0518 mL 0.2588 mL 0.5175 mL 1.0351 mL 1.2939 mL
100 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.5175 mL 0.6469 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SU 16f

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.[Pubmed:10602697]

J Med Chem. 1999 Dec 16;42(25):5120-30.

Receptor tyrosine kinases (RTKs) have been implicated as therapeutic targets for the treatment of human diseases including cancers, inflammatory diseases, cardiovascular diseases including arterial restenosis, and fibrotic diseases of the lung, liver, and kidney. Three classes of 3-substituted indolin-2-ones containing propionic acid functionality attached to the pyrrole ring at the C-3 position of the core have been identified as catalytic inhibitors of the vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) RTKs. Some of the compounds were found to inhibit the tyrosine kinase activity associated with isolated vascular endothelial growth factor receptor 2 (VEGF-R2) [fetal liver tyrosine kinase 1 (Flk-1)/kinase insert domain-containing receptor (KDR)], fibroblast growth factor receptor (FGF-R), and platelet-derived growth factor receptor (PDGF-R) tyrosine kinase with IC(50) values at nanomolar level. Thus, compound 1 showed inhibition against VEGF-R2 (Flk-1/KDR) and FGF-R1 tyrosine kinase activity with IC(50) values of 20 and 30 nM, respectively, while compound 16f inhibited the PDGF-R tyrosine kinase activity with IC(50) value of 10 nM. Structural models and structure-activity relationship analysis of these compounds for the target receptors are discussed. The cellular activities of these compounds were profiled using cellular proliferation assays as measured by bromodeoxyuridine (BrdU) incorporation. Specific and potent inhibition of cell growth was observed for some of these compounds. These data provide evidence that these compounds can be used to inhibit the function of these target receptors.

Description

SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. 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.

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