| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
EGFR (IC50 = 4.9 μM); ErbB2 (IC50 = 2.1 μM)
Tyrphostin AG-528 targets the epidermal growth factor receptor (EGFR) and ErbB2 (HER2). It acts as a potent inhibitor of the tyrosine kinase activity of these receptors. By blocking the kinase activity, the compound prevents the autophosphorylation of the receptors and the activation of downstream signaling pathways that promote cell proliferation and survival. The compound shows selectivity for EGFR and ErbB2 over other kinases. |
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| ln Vitro |
For the first time, Density Functional Theory (DFT) calculations in solvent water have been used to examine the relationship between the drug Tyrphostin AG528 and CNT(6,6-6) nanotube in this work. The complex stability of CNT(6,6-6)/Tyrphostin AG528 is largely dependent on intermolecular hydrogen bonds that form between the molecule Tyrphostin AG528's active position and the hydrogen atoms of the nanotube. The effects of Tyrphostin AG528's non-bonded interaction with the CNT(6,6-6) nanotube on the molecule's electrical characteristics, chemical shift tensors, and natural charge have also been identified. Tyrphostin AG528 is a molecule that donates electrons, and the CNT(6,6-6) nanotube acts as an electron acceptor at the complex CNT(6,6-6)/Tyrphostin AG528[2], according to the natural bond orbital (NBO) analysis.
In vitro, tyrphostin AG-528 has been shown to be a potent inhibitor of EGFR and ErbB2 kinase activity. It inhibits the proliferation of cancer cell lines that overexpress these receptors. The compound's activity is characterized by its low IC50 values for EGFR and ErbB2. |
| ln Vivo |
In vivo, tyrphostin AG-528 has been studied for its anti-cancer activity in animal models. Although specific in vivo efficacy data are less detailed, the compound's ability to inhibit EGFR and ErbB2 makes it a potential candidate for the treatment of cancers that depend on these signaling pathways.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for tyrphostin AG-528 involve measuring its direct inhibition of EGFR or ErbB2 kinase activity. The assay uses a purified recombinant kinase enzyme and a peptide substrate in the presence of ATP. The phosphorylation of the substrate is measured using a radioactive or fluorescent method. The compound is incubated with the enzyme and substrate, and the decrease in phosphorylation is measured to determine the IC50.
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| Cell Assay |
In vitro cell-based assays for tyrphostin AG-528 are performed using cancer cell lines that overexpress EGFR or ErbB2. Cells are treated with the compound, and cell viability and proliferation are assessed using standard assays. The compound's effects on receptor phosphorylation and downstream signaling pathways are analyzed by Western blotting.
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| Animal Protocol |
In vivo animal experiments for tyrphostin AG-528 are conducted using mouse xenograft models of cancer. Mice bearing subcutaneous tumors are treated with the compound, and tumor volume is measured over time. The compound's effects on tumor growth and survival are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tyrphostin AG-528 have been characterized to support its use as a research tool. The compound has a molecular weight of 306.32 and a formula of C₁₈H₁₄N₂O₃. It is soluble in DMSO. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tyrphostin AG-528 are typical of a research compound. It is generally well-tolerated at effective doses. The safety profile is being evaluated in the context of its use as a research tool to study EGFR and ErbB2 signaling.
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| References | |
| Additional Infomation |
Other information: Tyrphostin AG-528 is a research compound used to study the role of EGFR and ErbB2 in cancer. It is available from chemical suppliers for preclinical research purposes.
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| Molecular Formula |
C18H14N2O3
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|---|---|
| Molecular Weight |
306.321
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| Exact Mass |
306.1
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| Elemental Analysis |
C, 70.58; H, 4.61; N, 9.15; O, 15.67
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| CAS # |
133550-49-9
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| Related CAS # |
133550-49-9
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| PubChem CID |
1838043
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| Appearance |
Light yellow to yellow solid powder
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| Melting Point |
215 °C
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| LogP |
2.659
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C(/C#N)=C\C1C=CC(=C(C=1)O)O)N1C2C=CC=CC=2CC1
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| InChi Key |
MYKCTDWWIWGLHW-NTEUORMPSA-N
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| InChi Code |
InChI=1S/C18H14N2O3/c19-11-14(9-12-5-6-16(21)17(22)10-12)18(23)20-8-7-13-3-1-2-4-15(13)20/h1-6,9-10,21-22H,7-8H2/b14-9+
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| Chemical Name |
(E)-2-(2,3-dihydroindole-1-carbonyl)-3-(3,4-dihydroxyphenyl)prop-2-enenitrile
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| Synonyms |
Tyrphostin AG-528; Tyrphostin AG528; AG-528; AG 528; AG528; Tyrphostin B-66; Tyrphostin B66; Tyrphostin-B66; Tyrphostin AG 528
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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: 25~61 mg/mL (81.6~199.1 mM)
Water: ˂1 mg/mL Ethanol: ~5 mg/mL (~16.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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 (8.16 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 | 3.2646 mL | 16.3228 mL | 32.6456 mL | |
| 5 mM | 0.6529 mL | 3.2646 mL | 6.5291 mL | |
| 10 mM | 0.3265 mL | 1.6323 mL | 3.2646 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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