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| Targets |
ST-271 is a potent inhibitor of protein tyrosine kinase (PTK), a class of enzymes that catalyze the phosphorylation of tyrosine residues in proteins. By inhibiting PTK, it suppresses phospholipase D (PLD) activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 μM and 9 μM, respectively. The compound also inhibits the synthesis of inositol phosphate caused by FcγRII cross-linking. ST-271's mechanism of action involves the modulation of tyrosine kinase signaling pathways, which are important in cellular processes such as proliferation, differentiation, and immune responses.
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| ln Vitro |
Peptide phosphorylation in membrane preparations and permeabilized platelets is partially inhibited by ST271 [1]. In addition to totally blocking the synthesis of inositol phosphate caused by FcγRII cross-linking, ST271 (100 μM) significantly but subtly reduces the body's reaction to thrombin and U46619 [2].
In vitro, ST-271 partially inhibits peptide phosphorylation in membrane preparations and permeabilized platelets. It completely blocks the synthesis of inositol phosphate caused by FcγRII cross-linking. ST-271 (100 μM) significantly but subtly reduces the body's reaction to thrombin and U46619. It inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF with IC50s of 6.7 μM and 9 μM, respectively. These in vitro activities demonstrate that ST-271 effectively modulates tyrosine kinase and phospholipase D signaling pathways. |
| ln Vivo |
In vivo studies have demonstrated that ST-271, as a PTK inhibitor, can modulate signaling pathways involved in inflammation and immune responses. The compound's ability to inhibit phospholipase D activation suggests potential applications in conditions where PLD signaling is dysregulated. ST-271 has been studied in various preclinical models to evaluate its effects on tyrosine kinase-mediated signaling. Its tyrphostin-like structure and PTK inhibitory activity make it a valuable tool for studying the role of protein tyrosine kinases in cellular processes. However, detailed in vivo efficacy data for specific disease models are limited.
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| Enzyme Assay |
In vitro enzyme assays for ST-271 typically involve measuring the inhibition of protein tyrosine kinase (PTK) activity using purified enzymes or membrane preparations. Peptide phosphorylation assays are performed in the presence of varying concentrations of the compound to determine the IC50 values. ST-271 inhibits PTK activity with IC50s of 6.7 μM (fMet-Leu-Phe-stimulated) and 9 μM (PAF-stimulated). The compound's ability to inhibit phospholipase D (PLD) activation can also be assessed using enzymatic assays. These non-cellular assays confirm the compound's mechanism of action as a PTK inhibitor.
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| Cell Assay |
In vitro cellular assays for ST-271 typically involve treating cells such as platelets or leukocytes with the compound and measuring downstream effects on signaling pathways. Peptide phosphorylation in permeabilized platelets is partially inhibited by ST-271. The compound completely blocks the synthesis of inositol phosphate caused by FcγRII cross-linking. ST-271 (100 μM) reduces the body's reaction to thrombin and U46619. These cell-based assays demonstrate that ST-271 effectively modulates tyrosine kinase and phospholipase D signaling in a cellular context.
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| Animal Protocol |
In vivo animal models for ST-271 may include models of inflammation, immune response, or cancer, where tyrosine kinase signaling plays a role. The compound is typically administered by appropriate routes (e.g., intraperitoneal or oral) at doses optimized for the specific model. Efficacy is assessed by measuring biomarkers of tyrosine kinase activity or disease progression. However, detailed animal protocol information for ST-271 is limited in the available literature. The compound is primarily used as a research tool for studying PTK signaling pathways.
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| ADME/Pharmacokinetics |
ST-271 has a molecular weight of 272.34 g/mol and a molecular formula of C16H20N2O2. It is soluble in DMSO at concentrations ≥ 110 mg/mL. The compound is typically stored as a powder at -20°C for up to 3 years or in solution at -80°C for 6 months. Its chemical name is (E)-2-cyano-3-[4-hydroxy-3,5-di(propan-2-yl)phenyl]prop-2-enamide. ST-271's physicochemical properties support its use in both in vitro and in vivo studies. The compound's solubility in DMSO facilitates its formulation for cellular and animal studies.
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| Toxicity/Toxicokinetics |
ST-271 is a protein tyrosine kinase (PTK) inhibitor with a well-characterized mechanism of action. As with any kinase inhibitor, potential toxicity may include off-target effects on other kinases and disruption of normal cellular signaling. The compound's safety profile should be evaluated in preclinical toxicology studies. ST-271 is for research use only and is not approved for human therapeutic use. Its tyrphostin-like structure is characteristic of a class of compounds known for their ability to inhibit tyrosine kinases.
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| References |
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| Additional Infomation |
ST-271 (CAS# 106392-48-7) is a potent inhibitor of protein tyrosine kinase (PTK) with a tyrphostin-like α-cyanoacrylamide core structure. It inhibits phospholipase D (PLD) activation stimulated by fMet-Leu-Phe and PAF with IC50s of 6.7 μM and 9 μM, respectively. ST-271 partially inhibits peptide phosphorylation in membrane preparations and permeabilized platelets. It completely blocks inositol phosphate synthesis caused by FcγRII cross-linking and reduces responses to thrombin and U46619. The compound is for research use only and is not approved for human therapeutic use. It is a valuable tool for studying tyrosine kinase and phospholipase D signaling pathways.
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| Molecular Formula |
C16H20N2O2
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| Molecular Weight |
272.34
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| Exact Mass |
272.152
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| CAS # |
106392-48-7
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| PubChem CID |
6439072
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.137g/cm3
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| Boiling Point |
468.4ºC at 760mmHg
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| Flash Point |
237.1ºC
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| Vapour Pressure |
2.14E-09mmHg at 25°C
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| Index of Refraction |
1.585
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| LogP |
4.18
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
413
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C1=CC(=CC(=C1O)C(C)C)/C=C(\C#N)/C(=O)N
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| InChi Key |
HMLQHJRJKQDTKW-LFYBBSHMSA-N
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| InChi Code |
InChI=1S/C16H20N2O2/c1-9(2)13-6-11(5-12(8-17)16(18)20)7-14(10(3)4)15(13)19/h5-7,9-10,19H,1-4H3,(H2,18,20)/b12-5+
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| Chemical Name |
(E)-2-cyano-3-[4-hydroxy-3,5-di(propan-2-yl)phenyl]prop-2-enamide
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| Synonyms |
ST 271; ST271; ST-271
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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 : ≥ 110 mg/mL (~403.91 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 | 3.6719 mL | 18.3594 mL | 36.7188 mL | |
| 5 mM | 0.7344 mL | 3.6719 mL | 7.3438 mL | |
| 10 mM | 0.3672 mL | 1.8359 mL | 3.6719 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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