| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
WAY-272077 targets sphingosine kinase 1 (SphK1) and sphingosine kinase 2 (SphK2), the enzymes responsible for the phosphorylation of sphingosine to the pleiotropic lipid mediator sphingosine-1-phosphate (S1P). S1P plays critical roles in cell proliferation, survival, migration, and inflammation. By inhibiting SphK1/2, WAY-272077 reduces S1P production, making it a valuable tool for studying S1P signaling and its role in cancer and inflammatory diseases.
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| ln Vitro |
SphK1&2-IN-1 (compound 40) inhibits SphK1 and SphK2 by 14.3% and 26.5%, respectively, at a concentration of 10 μM [1]. The thermal stability of SphK1&2-IN-1 (Compound W4) (1-100 μM) is good [1].
In vitro, WAY-272077 is a dual inhibitor of SphK1 and SphK2. It functions as a synthetic aminothiazole derivative that inhibits the phosphorylation of sphingosine to S1P. These in vitro properties make WAY-272077 a valuable tool for studying S1P signaling and its role in cell proliferation, survival, migration, and inflammation. Quantitative in vitro data such as IC50 values are available from biochemical assays. |
| ln Vivo |
In vivo, WAY-272077 is a haemostatic agent, suggesting potential applications in coagulation and thrombosis research. As a dual SphK1/2 inhibitor, it may modulate S1P levels and affect vascular function and inflammation. However, detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro enzyme assay for WAY-272077 involves measuring its inhibition of SphK1 and SphK2 enzymatic activity. Recombinant SphK1 or SphK2 is incubated with the compound at various concentrations in the presence of sphingosine and ATP. Enzyme activity is measured by quantifying the production of S1P using mass spectrometry, HPLC, or radiolabeled assays. The IC50 for SphK1/2 inhibition is calculated from dose-response curves.
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| Cell Assay |
The in vitro cell-based assay for WAY-272077 involves culturing cells that express SphK1 and SphK2 and treating them with the compound to assess effects on S1P production and downstream signaling. Cells are treated with WAY-272077 at various concentrations, and S1P levels in cell lysates or conditioned media are measured by ELISA or mass spectrometry. Downstream signaling pathways, such as AKT, ERK, and STAT3 phosphorylation, are assessed by Western blot. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for WAY-272077 have not been extensively reported. If conducted, such studies might involve mouse models of cancer, inflammation, or thrombosis. WAY-272077 would be administered orally or intraperitoneally, and tumor growth, inflammatory markers, or thrombus formation would be assessed. Standard protocols for these models would be employed. No specific data are available.
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| ADME/Pharmacokinetics |
WAY-272077 has a molecular weight of 290.34 and a molecular formula of C14H14N2O3S. It is a synthetic aminothiazole derivative and a dual inhibitor of SphK1 and SphK2. The compound is soluble in DMSO (10 mM) 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 WAY-272077 has not been systematically evaluated. As a dual SphK1/2 inhibitor that reduces S1P production, its primary safety concerns would relate to effects on cell proliferation, survival, and immune function. 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.
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| References |
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| Additional Infomation |
WAY-272077 is a research compound and has not been approved for clinical use. It is a dual inhibitor of SphK1 and SphK2, also known as SphK1&2-IN-1, that functions as a synthetic aminothiazole derivative. WAY-272077 inhibits the phosphorylation of sphingosine to S1P and is a haemostatic agent. It is a valuable tool for studying S1P signaling in cancer, inflammation, and thrombosis research.
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| Molecular Formula |
C14H14N2O3S
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|---|---|
| Molecular Weight |
290.34
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| Exact Mass |
290.07
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| Elemental Analysis |
C, 57.92; H, 4.86; N, 9.65; O, 16.53; S, 11.04
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| CAS # |
1415662-57-5
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| PubChem CID |
897895
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
351
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NC1=NC=CS1)(=O)/C=C/C1=CC=C(OC)C(OC)=C1
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| InChi Key |
SMRXKMFZQYOXSX-GQCTYLIASA-N
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| InChi Code |
InChI=1S/C14H14N2O3S/c1-18-11-5-3-10(9-12(11)19-2)4-6-13(17)16-14-15-7-8-20-14/h3-9H,1-2H3,(H,15,16,17)/b6-4+
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| Chemical Name |
(2E)-3-(3,4-Dimethoxyphenyl)-N-2-thiazolyl-2-propenamide
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| Synonyms |
WAY-272077; WAY272077; WAY 272077;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.4442 mL | 17.2212 mL | 34.4424 mL | |
| 5 mM | 0.6888 mL | 3.4442 mL | 6.8885 mL | |
| 10 mM | 0.3444 mL | 1.7221 mL | 3.4442 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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