AG-1296

• CAT Number: I001482
• CAS Number: 146535-11-7
• Molecular Formula: C16H14N2O2
• Molecular Weight: 266.3
• Purity: ≥95%
• Target: PDGFR
• Solubility: Soluble in DMSO, not in water
• Storage: -20°C
• IUPAC Name: 6,7-dimethoxy-2-phenylquinoxaline
• InChI: InChI=1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
• InChIKey: QNOXYUNHIGOWNY-UHFFFAOYSA-N
• SMILES: COC1=C(C=C2C(=C1)N=CC(=N2)C3=CC=CC=C3)OC

Tyrphostin AG 1296（Cat No.:I001482） is a potent inhibitor of platelet-derived growth factor receptor (PDGFR) signaling. It exhibits an inhibitory concentration (IC50) range of 0.3-0.5 μM against PDGFR, effectively blocking its activity. However, it does not display inhibitory activity against epidermal growth factor receptor (EGFR). This selectivity makes Tyrphostin AG 1296 a valuable tool in studying the specific role of PDGFR signaling in cellular processes and as a potential therapeutic agent targeting PDGFR-related diseases, such as certain types of cancer and fibrotic disorders.

Reference

1:Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells. Li Y, Li Y, Liu Q, Wang A.Onco Targets Ther. 2015 May 14;8:1043-51. doi: 10.2147/OTT.S70691. eCollection 2015. PMID: 25999739 Free PMC Article2:Enhanced antitumor effect of YM872 and AG1296 combination treatment on human glioblastoma xenograft models. Watanabe T, Ohtani T, Aihara M, Ishiuchi S.J Neurosurg. 2013 Apr;118(4):838-45. doi: 10.3171/2012.11.JNS12362. Epub 2013 Jan 11. PMID: 23311938 3:Cytostatic and cytotoxic effects of tyrphostin AG1296 on RMS cells. Lasota M, Klein A, Balwierz W.Contemp Oncol (Pozn). 2012;16(1):1-5. doi: 10.5114/wo.2012.27329. Epub 2012 Feb 29. PMID: 23788847 Free PMC Article4:VEGF/KDR loop is a target of AG1296 in acute myeloid leukaemia showing FLT3-internal tandem duplications. Torres LA, Barbarroja N, Dorado G, Velasco F, López-Pedrera C.Br J Haematol. 2009 Jun;145(6):836-8. doi: 10.1111/j.1365-2141.2009.07673.x. Epub 2009 Apr 8. No abstract available. PMID: 19388942 5:Constitutive activation of c-kit by the juxtamembrane but not the catalytic domain mutations is inhibited selectively by tyrosine kinase inhibitors STI571 and AG1296. Ueda S, Ikeda H, Mizuki M, Ishiko J, Matsumura I, Tanaka H, Shibayama H, Sugahara H, Takai E, Zhang X, Machii T, Kanakura Y.Int J Hematol. 2002 Dec;76(5):427-35. PMID: 12512837 6:Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296. Kovalenko M, Rönnstrand L, Heldin CH, Loubtchenkov M, Gazit A, Levitzki A, Böhmer FD.Biochemistry. 1997 May 27;36(21):6260-9. PMID: 9174341