Tyrphostin AG 1296 (Synonyms: Tyrphostin AG1296) |
| Katalog-Nr.GC13045 |
Tyrphostin AG 1296 ist ein potenter und selektiver Inhibitor des Thrombozyten-Wachstumsfaktor-Rezeptors (PDGFR) mit einem IC50-Wert von 0,8 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 146535-11-7
Sample solution is provided at 25 µL, 10mM.
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Tyrphostin AG 1296 is a selective inhibitor of platelet-derived growth factor receptor (PDGFR) with IC50 value of 0.3μM-0.5μM [1].
Tyrphostin AG 1296 is an ATP-competitive inhibitor of PDGFR. It binds to PDGFR, causing a conformational change at the ATP-binding site. In the in vitro assay, it potently inhibits the ligand-induced autophosphorylation of PDGF receptor in Swiss 3T3 cell membranes. Tyrphostin AG 1296 does not affect the EGF receptor when the concentration is up to 100μM. Tyrphostin AG 1296 also inhibits the mitogenesis induced by PDGF but not EGF or insulin. It reversibly inhibits PDGF-induced DNA synthesis with a mean IC50 value of 1.5μM. Besides that, tyrphostin AG 1296 inhibits PDGF-induced cell growth with IC50 value of 3.2μM in Swiss 3T3 cells [1, 2].
References:
[1] Kovalenko M, Gazit A, Böhmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Research, 1994, 54(23): 6106-6114.
[2] Kovalenko M, Rönnstrand L, Heldin C H, et al. Phosphorylation site-specific inhibition of platelet-derived growth factor β-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Biochemistry, 1997, 36(21): 6260-6269.
| Cell experiment [1]: | |
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Cell lines |
Swiss 3T3 cells, porcine aortic endothelial cells, sis-transformed cells |
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Preparation method |
The solubility of this compound in DMSO is > 6.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
6-8 h |
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Applications |
AG1296 (0.1-5 μM) dose-dependently inhibited the activity of PDGF receptor kinase in Swiss 3T3 cell membranes. AG1296 inhibited PDGF receptor autophosphorylation with an IC50 of 0.3-0.5 μM. AG1296 was also highly inhibitory towards PDGF-induced mitogenesis. AG1296 inhibited the mitogenic effect of basic FGF on Swiss 3D cells, albeit with an IC50 of 12.3 ± 3.1 μM. AG1296 potently inhibited PDGF-induced cell growth (IC50: 3.2 μM). In porcine aortic endothelial cells, AG1296 inhibited autophosphorylation of both human PDGFα- and PDGFβ-receptor and inhibited equipotently PDGFα- and PDGFβ-receptor -dependent DNA synthesis in cells transfected with either receptor. AG1296 (5-50 μM) potently inhibited the growth of the sis-transformed NIH 3T3 cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Kovalenko M, Gazit A, Bhmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation[J]. Cancer Research, 1994, 54(23): 6106-6114. | |
| Cas No. | 146535-11-7 | SDF | |
| Überlieferungen | Tyrphostin AG1296 | ||
| Chemical Name | 6,7-dimethoxy-2-phenylquinoxaline | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC | ||
| Formula | C16H14N2O2 | M.Wt | 266.29 |
| Löslichkeit | ≥ 6.65mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7553 mL | 18.7765 mL | 37.553 mL |
| 5 mM | 0.7511 mL | 3.7553 mL | 7.5106 mL |
| 10 mM | 0.3755 mL | 1.8777 mL | 3.7553 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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