| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg |
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| Targets |
SU-5616 targets tyrosine kinases, particularly c-Met/HGFR, a receptor tyrosine kinase that plays critical roles in cell proliferation, migration, and survival. By modulating tyrosine kinase signaling pathways, SU-5616 regulates abnormal cell proliferation. The compound's activity against c-Met suggests potential applications in cancer research, as c-Met is frequently dysregulated in various cancers.
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| ln Vitro |
In vitro, SU-5616 potentially modulates tyrosine kinase signal transduction and regulates abnormal cell proliferation. It is an organic compound with activity against tyrosine kinases, including c-Met/HGFR. These in vitro properties make SU-5616 a valuable tool for studying tyrosine kinase-mediated signaling pathways and their roles in cancer cell proliferation. Quantitative in vitro data such as IC50 values are not readily available from publicly accessible sources.
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| ln Vivo |
In vivo activity of SU-5616 has not been extensively reported. As a tyrosine kinase modulator with activity against c-Met, it may have potential for treating cancers driven by aberrant tyrosine kinase signaling. However, detailed in vivo efficacy data are limited in publicly available sources. The compound is primarily used as a research tool for studying tyrosine kinase pathways.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for SU-5616 typically involves measuring its inhibition of tyrosine kinase activity, particularly c-Met/HGFR. The compound is incubated with recombinant c-Met enzyme in the presence of ATP and a peptide substrate. Kinase activity is measured using a luminescent or fluorescence-based assay (e.g., ADP-Glo or TR-FRET) to determine IC50 values. Selectivity profiling against other tyrosine kinases can be performed to confirm specificity.
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| Cell Assay |
The in vitro cell-based assay for SU-5616 involves culturing cancer cell lines that are dependent on tyrosine kinase signaling for proliferation, such as those with c-Met amplification or overexpression. Cells are treated with SU-5616 at various concentrations, and cell viability is assessed using MTT, CellTiter-Glo, or SRB assays to determine IC50 values. Downstream signaling pathways, such as AKT and ERK phosphorylation, can be assessed by Western blot to confirm target inhibition.
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| Animal Protocol |
In vivo animal studies for SU-5616 have not been extensively reported. If conducted, such studies might involve mouse xenograft models of c-Met-driven cancers, where SU-5616 is administered orally or intraperitoneally and tumor growth is monitored. Standard protocols for xenograft studies would be employed. No specific data are available from publicly accessible sources.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of SU-5616 have not been extensively characterized. As a small molecule with a molecular weight of 261.73 and a molecular formula of C13H8ClNOS, it is expected to have moderate oral bioavailability. The compound is soluble in DMSO and can be formulated for in vivo administration. Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SU-5616 has not been systematically evaluated. As a research compound targeting tyrosine kinases, its primary safety concerns would relate to on-target effects on normal cell proliferation and survival. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available from publicly accessible sources.
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| References | |
| Additional Infomation |
SU-5616 is a research compound and has not been approved for clinical use. It is an organic compound that modulates tyrosine kinase signal transduction, particularly targeting c-Met/HGFR, and regulates abnormal cell proliferation. SU-5616 is also known as WAY-608241 and 5-chloro-3-(thiophen-2-ylmethylene)indolin-2-one. It is a valuable tool for studying tyrosine kinase-mediated signaling in cancer research.
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| Molecular Formula |
C13H8NOSCL
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|---|---|
| Molecular Weight |
261.727
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| Exact Mass |
261
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| Elemental Analysis |
C, 59.66; H, 3.08; Cl, 13.54; N, 5.35; O, 6.11; S, 12.25
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| CAS # |
186611-58-5
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| PubChem CID |
2357047
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
357
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC2=C(/C(=C/C3=CC=CS3)/C(=O)N2)C=1
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| InChi Key |
ZYHHCVFJHNWKDY-XFFZJAGNSA-N
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| InChi Code |
InChI=1S/C13H8ClNOS/c14-8-3-4-12-10(6-8)11(13(16)15-12)7-9-2-1-5-17-9/h1-7H,(H,15,16)/b11-7-
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| Chemical Name |
(Z)-5-chloro-3-(thiophen-2-ylmethylene)indolin-2-one
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| Synonyms |
SU-5616; SU 5616; SU5616;
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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 : ~15.62 mg/mL (~59.68 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 | 3.8207 mL | 19.1037 mL | 38.2073 mL | |
| 5 mM | 0.7641 mL | 3.8207 mL | 7.6415 mL | |
| 10 mM | 0.3821 mL | 1.9104 mL | 3.8207 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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