| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
AG 112 targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds to the ATP-binding site of EGFR, preventing receptor autophosphorylation and subsequent phosphorylation of downstream signaling molecules. This inhibition interferes with growth factor signaling pathways that regulate cell proliferation, differentiation, and survival. In cell-free assays, AG-112 inhibits EGFR-catalyzed phosphorylation of poly(GAT) with an IC50 of 0.125 µM.
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| ln Vitro |
In vitro, AG 112 inhibits EGFR-catalyzed phosphorylation with an IC50 of 0.125 µM in cell-free assays. It also inhibits calcineurin phosphatase activity. As an EGFR tyrosine kinase inhibitor, it prevents receptor phosphorylation and downstream signaling. The compound shows potent and selective inhibition of EGFR phosphorylation.
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| ln Vivo |
In vivo activity data for AG 112 are not extensively detailed in the available literature. As an EGFR inhibitor, the compound would be expected to inhibit EGFR-driven tumor growth in vivo. Specific in vivo efficacy data are not reported.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for AG 112 involve EGFR kinase activity assays. IC50 of 0.125 µM is determined by measuring inhibition of EGFR-catalyzed phosphorylation of poly(GAT). Calcineurin phosphatase inhibition is also assessed. ATP-binding site competition is confirmed through kinetic analysis.
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| Cell Assay |
In vitro cell-based assays for AG 112 use EGFR-expressing cancer cell lines. Cells are treated with the compound, and EGFR phosphorylation is assessed by Western blot. Cell proliferation is measured using standard viability assays. Inhibition of downstream signaling pathways (e.g., MAPK, PI3K/AKT) is evaluated.
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| Animal Protocol |
In vivo animal studies for AG 112 are not detailed in the available literature. As an EGFR inhibitor, typical in vivo evaluation would involve xenograft mouse models bearing EGFR-driven tumors. Tumor-bearing mice would be treated with AG 112, and tumor growth inhibition would be monitored.
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| ADME/Pharmacokinetics |
AG 112 (Tyrphostin AG 112) has a molecular formula of C13H8N4O and a molecular weight of 236.23 g/mol. The IUPAC name is (Z)-2-amino-4-(4-hydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile. It is soluble in DMSO at 125 mg/mL (529.15 mM). Purity is >98% (HPLC). Storage: dry, dark, at 0-4°C for short term or -20°C for long term.
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| Toxicity/Toxicokinetics |
Specific toxicological data for AG 112 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As an EGFR tyrosine kinase inhibitor, potential toxicities would relate to inhibition of EGFR signaling in normal tissues, though formal toxicological profiles are not reported.
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| References | |
| Additional Infomation |
2-Amino-4-(4-hydroxyphenyl)but-1,3-diene-1,1,3-trionitrile belongs to the phenolic class of compounds. Tyrosine kinase inhibitor A48 is a member of the tyrosine kinase inhibitor family and inhibits epidermal growth factor receptor tyrosine kinase. (NCI)
AG 112 (CAS 144978-82-5), also known as Tyrphostin AG 112, is an inhibitor of EGFR phosphorylation with an IC50 of 0.125 µM in cell-free assays. It binds to the ATP-binding site of EGFR and inhibits downstream signaling. The compound also inhibits calcineurin phosphatase. No clinical trial data are available. |
| Molecular Formula |
C7H4N4.C6H6O
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|---|---|
| Molecular Weight |
238.2447
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| Exact Mass |
236.07
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| CAS # |
144978-82-5
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| PubChem CID |
5328804
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.259
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
505
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#CC(/C(=C(\C#N)/C#N)/N)=C.OC1C=CC=CC=1
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| InChi Key |
DXVJRTIPBNBLLB-BJMVGYQFSA-N
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| InChi Code |
InChI=1S/C13H8N4O/c14-6-10(13(17)11(7-15)8-16)5-9-1-3-12(18)4-2-9/h1-5,18H,17H2/b10-5+
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| Chemical Name |
(3Z)-2-amino-4-(4-hydroxyphenyl)buta-1,3-diene-1,1,3-tricarbonitrile
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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 : ~125 mg/mL (~529.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.80 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 (8.80 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 | 4.1974 mL | 20.9872 mL | 41.9745 mL | |
| 5 mM | 0.8395 mL | 4.1974 mL | 8.3949 mL | |
| 10 mM | 0.4197 mL | 2.0987 mL | 4.1974 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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