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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.
Physicochemical Properties
| Molecular Formula | C10H7NO4 |
| Molecular Weight | 205.17 |
| Exact Mass | 205.038 |
| Elemental Analysis | C, 53.40; H, 4.03; Cl, 7.88; F, 8.45; N, 15.57; O, 10.67 |
| CAS # | 122520-79-0 |
| Related CAS # | 122520-79-0 |
| PubChem CID | 5328793 |
| Appearance | Solid powder |
| Density | 1.559g/cm3 |
| Boiling Point | 465.6ºC at 760mmHg |
| Flash Point | 235.4ºC |
| Vapour Pressure | 1.8E-09mmHg at 25°C |
| Index of Refraction | 1.717 |
| LogP | 1.089 |
| 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 |
| InChi Key | CJMWBHLWSMKFSM-XVNBXDOJSA-N |
| 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+ |
| Chemical Name | (E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoic acid |
| Synonyms | Tyrphostin AG30; AG 30; AG-30; AG30 |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | EGFR |
| References |
[1]. The effect of tyrosine-specific protein phosphorylation on the assembly of adherens-type junctions. EMBO J. 1992 May;11(5):1733-42. [2]. Distinct roles of the receptor tyrosine kinases c-ErbB and c-Kit in regulating the balance between erythroid cell proliferation and differentiation. Cell Growth Differ. 1997 May;8(5):481-93. [3]. Epidermal growth factor induces WISP-2/CCN5 expression in estrogen receptor-alpha-positive breast tumor cells through multiple molecular cross-talks. Mol Cancer Res. 2005 Mar;3(3):151-62. |
Solubility Data
| Solubility (In Vitro) |
DMSO: ~41 mg/mL (199.8 mM) Ethanol: ~3 mg/mL (14.6 mM) |
| 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 |