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| Targets |
SU16F specifically targets the platelet-derived growth factor receptor beta (PDGFRβ), a receptor tyrosine kinase that plays a critical role in cell proliferation, migration, and angiogenesis. By selectively inhibiting PDGFRβ, SU16F blocks the downstream signaling pathways activated by PDGF binding, including the PI3K/AKT and MAPK/ERK pathways. Its high selectivity for PDGFRβ over other kinases such as VEGFR2, FGFR1, and EGFR makes it a valuable tool for dissecting PDGFRβ-specific biological functions without off-target effects.
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| ln Vitro |
Pretreatment with SU16f (20 μM; 8 hours) prevents GC-MSC-CM from promoting the growth of SGC-7901 cells [1]. GC-MSC-CM significantly reduced PDGFRβ activation in SGC-7901 when SU16f (20 μM) was applied for 8 hours. E-cadherin was upregulated and vimentin, N-cadherin, and α-SMA were downregulated following SU16f pretreatment. In SGC-7901 cells, SU16f pretreatment led to GC-MSC-CM upregulating Bax expression and downregulating p-AKT, Bcl-xl, and Bcl-2 levels [1].
In vitro, SU16F (20 μM; 8 hours) significantly inhibits PDGFRβ activation in SGC-7901 gastric cancer cells induced by gastric cancer-derived mesenchymal stem cell conditioned medium (GC-MSC-CM). Pretreatment with SU16F effectively blocks the proliferative and migratory促进作用 of GC-MSC-CM on SGC-7901 cells. Mechanistically, SU16F pretreatment leads to downregulation of p-AKT, Bcl-xl, and Bcl-2 levels, while upregulating Bax expression. Additionally, it causes upregulation of E-cadherin and downregulation of N-cadherin, vimentin, and α-SMA, indicating a reversal of epithelial-mesenchymal transition (EMT). |
| ln Vivo |
In vivo, SU16F has been used to study the role of PDGFRβ signaling in tumor progression and metastasis. By inhibiting PDGFRβ, SU16F blocks the promoting effect of tumor microenvironment components, such as cancer-associated fibroblasts and mesenchymal stem cells, on cancer cell proliferation and migration. While specific in vivo efficacy data are limited, the compound's potent and selective PDGFRβ inhibition makes it a valuable tool for validating PDGFRβ as a therapeutic target in various disease models, including gastric cancer and fibrosis.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SU16F typically involve evaluating its inhibitory activity against purified PDGFRβ kinase using radiometric or fluorescence-based kinase activity assays. The compound is incubated with the kinase, ATP, and a substrate peptide, and the phosphorylation of the substrate is measured. IC₅₀ values are determined by plotting the percentage of inhibition against the log of compound concentration. Selectivity profiling is performed by testing SU16F against a panel of related kinases, such as VEGFR2, FGFR1, and EGFR.
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: SGC-7901 cells in GC-MSC/SGC-7901 co-culture system Tested Concentrations: 20 μM Incubation Duration: 8 hrs (hours) Experimental Results: Inhibition of the promotion effect of GC-MSC-CM on SGC-7901 cells proliferation. Western Blot Analysis[1] Cell Types: SGC-7901 Cell Tested Concentrations: 20 μM Incubation Duration: 8 hrs (hours) Experimental Results: GC-MSC-CM Dramatically eliminated the activation of PDGFRβ in SGC-7901, resulting in upregulation of E-cadherin and downregulation of N-calcium Mucin, vimentin, and α-SMA. For in vitro cell-based assays, SU16F is dissolved in DMSO and applied to cultured cells such as SGC-7901 gastric cancer cells at concentrations ranging from 1-20 µM. Cells are typically pretreated with SU16F for 8 hours prior to stimulation with GC-MSC-CM. The effects on cell proliferation, migration, and signaling pathways are assessed using MTT assays, wound healing assays, and Western blotting for markers such as PDGFRβ phosphorylation, AKT, Bcl-2 family proteins, and EMT markers. |
| Animal Protocol |
In vivo animal studies for SU16F are typically conducted in mouse xenograft models of cancer. The compound is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Efficacy is evaluated by measuring tumor volume, tumor weight, and molecular markers of PDGFRβ signaling in tumor tissues. However, detailed in vivo pharmacokinetic and efficacy data for SU16F are not extensively published in the public domain.
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| ADME/Pharmacokinetics |
SU16F has a molecular formula of C₂₄H₂₂N₂O₃ and a molecular weight of 386.44 g/mol. It is soluble in DMSO and is typically stored as a powder at -20°C for long-term stability. The compound has a LogP of 4.946, indicating moderate lipophilicity. It is supplied with a purity of ≥98% for research use only.
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| Toxicity/Toxicokinetics |
SU16F is considered to have a manageable toxicity profile for research use. As a selective kinase inhibitor, it is not intended for human therapeutic use and is classified as a research chemical. Appropriate safety precautions, including the use of personal protective equipment, should be followed when handling the compound. No significant acute toxicity has been reported in preclinical studies at the doses typically used for research.
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| References |
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| Additional Infomation |
SU16F is a potent and selective PDGFRβ inhibitor used as a research tool to study PDGFRβ signaling in cancer, fibrosis, and other diseases. Its discovery and characterization have contributed to the understanding of PDGFRβ as a therapeutic target. SU16F is not approved for clinical use and is intended for research purposes only. It is supplied by various research chemical suppliers for non-human use.
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| Molecular Formula |
C24H22N2O3
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| Molecular Weight |
386.443086147308
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| Exact Mass |
386.163
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| Elemental Analysis |
C, 74.59; H, 5.74; N, 7.25; O, 12.42
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| CAS # |
251356-45-3
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| PubChem CID |
5329150
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| Appearance |
Yellow to orange solid powder
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| Density |
1.292±0.06 g/cm3(Predicted)
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| Boiling Point |
661.7±55.0 ℃(Predicted)
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| LogP |
4.946
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
655
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C2/C(=C/C3NC(C)=C(CCC(=O)O)C=3C)/C(=O)NC2=CC(C2C=CC=CC=2)=C1
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| InChi Key |
APYYTEJNOZQZNA-MOSHPQCFSA-N
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| InChi Code |
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-
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| Chemical Name |
3-[2,4-dimethyl-5-[(Z)-(2-oxo-6-phenyl-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
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| Synonyms |
SU16F; SU-16F; SU 16F;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~129.39 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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