| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Tyrphostin B44, (+) enantiomer targets the epidermal growth factor receptor (EGFR) kinase. It acts as an inhibitor, blocking the kinase activity of EGFR. By inhibiting EGFR, it has anti-tumor activity. It has also shown antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity.
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|---|---|
| ln Vitro |
(+)-Tyrphostin B44 (Tyrphostin AG 835) (Compound B50) has an EC50 value of 3.12, 12.5, and 12.5 µM for CALO, INBL, and HeLa cells, respectively, and reduces cell survival at concentrations ranging from 0-100 µM [1].
In vitro, Tyrphostin B44, (+) enantiomer is an EGFR kinase inhibitor with an IC50 of 0.86 μM. It has shown antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells. The compound has anti-tumor activity. |
| ln Vivo |
In vivo activity data for Tyrphostin B44, (+) enantiomer are not extensively detailed in the available sources. As an EGFR inhibitor, it has potential for cancer research. Its antiviral activity suggests potential for in vivo studies in models of viral infection.
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| Enzyme Assay |
The in vitro enzyme assay for Tyrphostin B44, (+) enantiomer involves measuring the inhibition of EGFR kinase activity. Recombinant EGFR is incubated with a substrate peptide and ATP in the presence of varying compound concentrations. The IC50 of 0.86 μM is determined by quantifying the reduction in substrate phosphorylation.
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| Cell Assay |
Cellular assays for Tyrphostin B44, (+) enantiomer are performed using cancer cell lines or virus-infected cells. Cells are treated with the compound at various concentrations. Cell viability is assessed using standard assays. EGFR phosphorylation is measured by Western blotting.
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| Animal Protocol |
In vivo animal studies for Tyrphostin B44, (+) enantiomer are not detailed in the available sources. The compound is a research tool for studying EGFR function. Specific animal models, dosing regimens, and efficacy data have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Tyrphostin B44, (+) enantiomer are not available in the provided sources. The compound has a molecular weight of 308.34 g/mol. It is soluble in DMSO. Specific PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for Tyrphostin B44, (+) enantiomer are not reported in the available sources. As a research compound, it is not intended for therapeutic use. Specific toxicological profiles have not been characterized.
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| References | |
| Additional Infomation |
Tyrphostin B50 is a member of the tyrosine kinase inhibitor family. It inhibits epidermal growth factor receptors and blocks metavanadate-induced respiratory burst in alveolar macrophages. (National Cancer Institute)
Tyrphostin B44, (+) enantiomer is a research compound for studying EGFR kinase function in cancer and viral infections. It is an EGFR inhibitor with an IC50 of 0.86 μM. The compound is available from commercial suppliers for research purposes only. |
| Molecular Formula |
C18H16N2O3
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|---|---|
| Molecular Weight |
308.33124
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| Exact Mass |
308.116
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| CAS # |
133550-37-5
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| PubChem CID |
5328769
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.299g/cm3
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| Boiling Point |
603ºC at 760mmHg
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| Melting Point |
146 °C
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| Flash Point |
318.5ºC
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| Vapour Pressure |
3.9E-15mmHg at 25°C
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| Index of Refraction |
1.66
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| LogP |
3.273
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
488
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(/C=C(\C#N)/C(N[C@@H](C)C2=CC=CC=C2)=O)=CC(O)=C(O)C=C1
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| InChi Key |
UMGQVUWXNOJOSJ-DGGAMASNSA-N
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| InChi Code |
InChI=1S/C18H16N2O3/c1-12(14-5-3-2-4-6-14)20-18(23)15(11-19)9-13-7-8-16(21)17(22)10-13/h2-10,12,21-22H,1H3,(H,20,23)/b15-9+/t12-/m0/s1
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| Chemical Name |
(E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-[(1S)-1-phenylethyl]prop-2-enamide
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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 : ≥ 100 mg/mL (~324.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2433 mL | 16.2164 mL | 32.4328 mL | |
| 5 mM | 0.6487 mL | 3.2433 mL | 6.4866 mL | |
| 10 mM | 0.3243 mL | 1.6216 mL | 3.2433 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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