A potent and selective inhibitor of PDGFR with IC50 of about 0.4 uM both in vitro and in cells.
Cat.No
DC21767
Name
AG-1296
Chemical Properties
CAS
146535-11-7
Formula
C16H14N2O2
MW
266.29
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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.
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