| Description: |
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[1][2][3]. |
| Target: |
PDGFRα
PDGFRβ |
| In Vivo: |
Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4]. Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4]. Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4]. Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4]. Cell Viability Assay[4] Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R) Concentration: 0.625, 1.25, 5, 20 μM Incubation Time: 72 h Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines. Apoptosis Analysis[4] Cell Line: A375R cells Concentration: 2.5, 5, 10, 20 μM Incubation Time: 48 h Result: Induced dramatic apoptosis in A375R cells. Western Blot Analysis[4] Cell Line: A375R cells Concentration: 5, 20 μM Incubation Time: 2 h Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β. |
| In Vitro: |
Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4]. Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4]. Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4]. Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4]. Cell Viability Assay[4] Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R) Concentration: 0.625, 1.25, 5, 20 μM Incubation Time: 72 h Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines. Apoptosis Analysis[4] Cell Line: A375R cells Concentration: 2.5, 5, 10, 20 μM Incubation Time: 48 h Result: Induced dramatic apoptosis in A375R cells. Western Blot Analysis[4] Cell Line: A375R cells Concentration: 5, 20 μM Incubation Time: 2 h Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β. |
| 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.
[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.
[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.
[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.
[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. |
