Tyrphostin AG1296
Based on 3 publication(s) in Google Scholar
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 146535-11-7
- Formula: C16H14N2O2
- Molecular Weight:266.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Publications Citing Use of MedChemExpress (MCE) Tyrphostin AG1296
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Biological Activity
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PDGFRα |
PDGFRβ |
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | CC50 |
1.36 μM
Compound: TYRPHOSTIN AG 1296 (AG 1296)
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
0.2 μM
Compound: TYRPHOSTIN AG 1296 (AG 1296)
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
| NIH3T3 | IC50 |
0.8 μM
Compound: 26
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Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells
Inhibitory activity against platelet-derived growth factor receptor tyrosine kinase in Swiss 3T3 cells
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[PMID: 8667360] |
Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4].
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Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4].
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Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4].
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Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PLX4032-resistant cell lines (A375R and SK-MEL-5R)
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Concentration:0.625, 1.25, 5, 20 μM
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Incubation Time:72 h
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Result:Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines.
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Cell Line:A375R cells
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Induced dramatic apoptosis in A375R cells.
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Cell Line:A375R cells
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Concentration:5, 20 μM
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Incubation Time:2 h
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Result:Inhibited phosphorylation of both PDGFR-α and PDGFR-β.
? Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nud/nud mice are injected with A375R cells[4]
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Dosage:40, 80 mg/kg
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Administration:I.p. daily for two weeks
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Result:Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
Chemical Information
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CAS No. 146535-11-7
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Appearance Solid
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Molecular Weight 266.29
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Formula C16H14N2O2
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Color Off-white to yellow
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SMILES
COC1=C(OC)C=C2N=CC(C3=CC=CC=C3)=NC2=C1
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Synonyms
AG1296
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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J Extracell Vesicles
Umbilical Cord-Mesenchymal Stromal Cell-Derived Extracellular Vesicles Target the Liver to Improve Neurovascular Health in Type 2 Diabetes With Non-Alcoholic Fatty Liver Disease. [Abstract]2025 Jul;14(7):e70125. PMID: 40620065 -
Phytomedicine
Glycyrol alleviates osteoporosis through dual modulation on osteoclastogenesis and osteogenesis by targeting Syk signaling pathway. [Abstract]2025 Mar:138:156429. PMID: 39939034 -
Bioengineered
Plin5 inhibits proliferation and migration of vascular smooth muscle cell through interacting with PGC-1α following vascular injury. [Abstract]2022 Apr;13(4):10665-10678. PMID: 35470759
Solvent & Solubility
DMSO : 33.33 mg/mL (125.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.39 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Gazit A, etm, al. Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. Comparative Study J Med Chem. 1996 May 24; 39(11): 2170-7. [Content Brief]
[2]. Kovalenko M, et, al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1; 54(23): 6106-14. [Content Brief]
[3]. Tse KF, et, al. Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitor. Leukemia. 2002 Oct; 16(10): 2027-36. [Content Brief]
[4]. Li Y, et, al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells. Onco Targets Ther. 2015 May 14; 8: 1043-51. [Content Brief]
[5]. Dong M, et, al. AG1296 enhances plaque stability via inhibiting inflammatory responses and decreasing MMP-2 and MMP-9 expression in ApoE-/- mice. Biochem Biophys Res Commun. 2017 Aug 5;489(4):426-431. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7553 mL | 18.7765 mL | 37.5530 mL | 93.8826 mL |
| 5 mM | 0.7511 mL | 3.7553 mL | 7.5106 mL | 18.7765 mL | |
| 10 mM | 0.3755 mL | 1.8777 mL | 3.7553 mL | 9.3883 mL | |
| 15 mM | 0.2504 mL | 1.2518 mL | 2.5035 mL | 6.2588 mL | |
| 20 mM | 0.1878 mL | 0.9388 mL | 1.8777 mL | 4.6941 mL | |
| 25 mM | 0.1502 mL | 0.7511 mL | 1.5021 mL | 3.7553 mL | |
| 30 mM | 0.1252 mL | 0.6259 mL | 1.2518 mL | 3.1294 mL | |
| 40 mM | 0.0939 mL | 0.4694 mL | 0.9388 mL | 2.3471 mL | |
| 50 mM | 0.0751 mL | 0.3755 mL | 0.7511 mL | 1.8777 mL | |
| 60 mM | 0.0626 mL | 0.3129 mL | 0.6259 mL | 1.5647 mL | |
| 80 mM | 0.0469 mL | 0.2347 mL | 0.4694 mL | 1.1735 mL | |
| 100 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.9388 mL |
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