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Tyrphostin AG30 (AG30) is a potent and selective inhibitor of EGFR tyrosine kinase. Tyrphostin AG30 (AG30) selectively prevents c-ErbB from inducing self-renewal in primary erythroblasts and prevents c-ErbB from activating STAT5.
| Targets |
EGFR
EGFR (epidermal growth factor receptor) tyrosine kinase – no IC50, Ki, EC50, or DC50 values are provided in the specified references [3]. Protein tyrosine kinases (PTKs) of the src family – no specific affinity or potency data are given [1]. |
|---|---|
| ln Vitro |
In RSV-transformed chicken lens cells maintained at the permissive temperature, treatment with AG30 at concentrations of 200 µM or higher resulted in the restoration of intercellular adherens junctions, as evidenced by the reappearance of P-Tyr- and N-cadherin-containing junctional structures. The effect was observed after 8 hours of incubation, and among various tyrphostins tested, AG30 was effective only at higher concentrations (≥200 µM) [1].
In MCF-7 human breast carcinoma cells (ER-α-positive, EGFR-positive), serum-starved cells were exposed to EGF (100 ng/mL) for 24 hours, which induced WISP-2/CCN5 mRNA expression by approximately 4.6-fold compared to untreated control. Co-treatment with AG30 at 100 μmol/L significantly reduced this EGF-induced up-regulation of WISP-2/CCN5 mRNA, as determined by Northern blot analysis. This inhibition confirmed that the effect of EGF on WISP-2/CCN5 expression is mediated through EGFR [3]. |
| Cell Assay |
For restoration of adherens junctions in RSV-transformed cells: Chicken lens cells transformed with a temperature-sensitive mutant of RSV were cultured at the permissive temperature (37°C) in DMEM containing 10% fetal calf serum. Various tyrphostins, including AG30, were added directly to the complete culture medium at final concentrations ranging from 25 to 200 µM. Stock solutions of tyrphostins were prepared in DMSO. The cells were incubated for 8 hours, after which they were fixed, permeabilized, and immunolabeled for P-Tyr or N-cadherin to assess junction formation. AG30 was effective in restoring cell-cell junctions at concentrations of 200 µM or higher [1].
For inhibition of EGF-induced WISP-2/CCN5 expression in MCF-7 cells: MCF-7 cells (approximately 70% confluent) were serum-deprived for 3 days to achieve an estrogen- and growth factor-free environment. The starved cells were then exposed to EGF (100 ng/mL) alone or in combination with AG30 (100 μmol/L) for 24 hours. Total RNA was extracted using the Trizol method, and Northern blot analysis was performed using a digoxigenin-labeled, PCR-generated probe specific for human WISP-2/CCN5. GAPDH was used as a loading control. AG30 treatment reduced the EGF-stimulated WISP-2/CCN5 mRNA level back towards the basal level [3]. |
| References |
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| Additional Infomation |
AG30 is one of several tyrphostins synthesized and tested for their ability to inhibit protein tyrosine kinases. In the concentration range used (25–200 µM), the various tyrphostins were reported to be non-toxic to cells [1].
The compound has been shown to act as a broad-spectrum PTK inhibitor, but among the tested tyrphostins, AG18 and AG82 were most effective at restoring junctions at relatively low concentrations, whereas AG30 required higher concentrations (≥200 µM) to achieve a similar effect in RSV-transformed lens cells [1]. In breast cancer research, AG30 is employed as a tool to block EGFR tyrosine kinase activity and to study downstream signaling events, such as the EGF-dependent induction of WISP-2/CCN5 gene expression [3]. |
| Molecular Formula |
C10H7NO4
|
|---|---|
| Molecular Weight |
205.17
|
| Exact Mass |
205.038
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| Elemental Analysis |
C, 53.40; H, 4.03; Cl, 7.88; F, 8.45; N, 15.57; O, 10.67
|
| CAS # |
122520-79-0
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| Related CAS # |
122520-79-0
|
| PubChem CID |
5328793
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| Appearance |
Solid powder
|
| Density |
1.559g/cm3
|
| Boiling Point |
465.6ºC at 760mmHg
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| Flash Point |
235.4ºC
|
| Vapour Pressure |
1.8E-09mmHg at 25°C
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| Index of Refraction |
1.717
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| LogP |
1.089
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
15
|
| Complexity |
328
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(/C(=C/C1C=CC(O)=C(O)C=1)/C(O)=O)#N
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| InChi Key |
CJMWBHLWSMKFSM-XVNBXDOJSA-N
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| InChi Code |
InChI=1S/C10H7NO4/c11-5-7(10(14)15)3-6-1-2-8(12)9(13)4-6/h1-4,12-13H,(H,14,15)/b7-3+
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| Chemical Name |
(E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoic acid
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| Synonyms |
Tyrphostin AG30; AG 30; AG-30; AG30
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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: ~41 mg/mL (199.8 mM)
Ethanol: ~3 mg/mL (14.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.14 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 20.8 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: ≥ 2.08 mg/mL (10.14 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 20.8 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 | 4.8740 mL | 24.3700 mL | 48.7401 mL | |
| 5 mM | 0.9748 mL | 4.8740 mL | 9.7480 mL | |
| 10 mM | 0.4874 mL | 2.4370 mL | 4.8740 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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