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Tyrphostin AG 1296
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, B?hmer A, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Research, 1994, 54(23): 6106-6114.
[2] Kovalenko M, R?nnstrand 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.
- 1. Siqun Xu, Jieya Wei, et al. "PDGF‐AA guides cell crosstalk between human dental pulp stem cells in vitro via the PDGFR‐α/PI3K/Akt axis." Int Endod J. 2024 May;57(5):549-565. PMID: 38332717
- 2. Zhang X, Zhao F, et al. "PDGF-mediated PI3K/AKT/β-catenin signaling regulates gap junctions in corpus cavernosum smooth muscle cells." Exp Cell Res. 2017 Nov 22. pii: S0014-4827(17)30627-4. PMID:29174980
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 266.29 |
| Cas No. | 146535-11-7 |
| Formula | C16H14N2O2 |
| Solubility | insoluble in H2O; ≥2.8 mg/mL in EtOH with ultrasonic; ≥6.65 mg/mL in DMSO |
| Chemical Name | 6,7-dimethoxy-2-phenylquinoxaline |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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. |
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| Description | Tyrphostin AG 1296 is a selective inhibitor of platelet-derived growth factor receptor (PDGFR) with IC50 value of 0.3 μM-0.5 μM. | |||||
| Targets | PDGFR | |||||
| IC50 | 0.3 μM-0.5 μM | |||||
Quality Control & MSDS
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