Date published: 2026-1-9

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AG-1296 (CAS 146535-11-7)

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Alternate Names:
6,7-Dimethoxy-3-phenylquinoxaline;Tyrphostin AG 1296
Application:
AG-1296 is a potent inhibitor of PDGFR kinase and c-Kit
CAS Number:
146535-11-7
Purity:
>98%
Molecular Weight:
266.29
Molecular Formula:
C16H14N2O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AG-1296 is a potent and selective inhibitor of PDGFR kinase (IC50= 0.4 muM) both in vitro and in cells (Swiss 3T3 cells). This compound also inhibits Bek (FGF receptor) tyrosine kinase and c-kit. Treatment of sis oncogene transfected NIH3T3 cells with AG-1296 reverses the transformed phenotype. It also induces apoptosis in a small-cell lung cancer cell line (H526). AG-1296 is an inhibitor of Tyrosine Kinase. AG-1296 is an inhibitor of PDGFR-alpha and PDGFR-beta.


AG-1296 (CAS 146535-11-7) References

  1. 5-hydroxytryptamine 2B receptor regulates cell-cycle progression: cross-talk with tyrosine kinase pathways.  |  Nebigil, CG., et al. 2000. Proc Natl Acad Sci U S A. 97: 2591-6. PMID: 10688905
  2. TGF-beta 1 induces proliferation in human renal fibroblasts via induction of basic fibroblast growth factor (FGF-2).  |  Strutz, F., et al. 2001. Kidney Int. 59: 579-92. PMID: 11168939
  3. The role of PDGF receptor inhibitors and PI3-kinase signaling in the pathogenesis of corneal neovascularization.  |  Dell, S., et al. 2006. Invest Ophthalmol Vis Sci. 47: 1928-37. PMID: 16639000
  4. Hepatic stellate cell protrusions couple platelet-derived growth factor-BB to chemotaxis.  |  Melton, AC. and Yee, HF. 2007. Hepatology. 45: 1446-53. PMID: 17465006
  5. Cyclic strain induces mouse embryonic stem cell differentiation into vascular smooth muscle cells by activating PDGF receptor beta.  |  Shimizu, N., et al. 2008. J Appl Physiol (1985). 104: 766-72. PMID: 18187612
  6. Combination of vascular endothelial growth factor receptor/platelet-derived growth factor receptor inhibition markedly improves the antiangiogenic efficacy for advanced stage mouse corneal neovascularization.  |  Chaoran, Z., et al. 2011. Graefes Arch Clin Exp Ophthalmol. 249: 1493-501. PMID: 21574021
  7. Fingolimod potentiates the effects of sunitinib malate in a rat breast cancer model.  |  Mousseau, Y., et al. 2012. Breast Cancer Res Treat. 134: 31-40. PMID: 22160641
  8. Tyrphostin AG 1296 induces glioblastoma cell apoptosis in vitro and in vivo.  |  Li, H., et al. 2015. Oncol Lett. 10: 3429-3433. PMID: 26788146
  9. Cross-talk between TGF-β and PDGFRα signaling pathways regulates the fate of stromal fibro-adipogenic progenitors.  |  Contreras, O., et al. 2019. J Cell Sci. 132: PMID: 31434718
  10. Small-molecule inhibitor - tyrphostin AG1296 regulates proliferation, survival and migration of rhabdomyosarcoma cells.  |  Lasota, M., et al. 2021. J Physiol Pharmacol. 72: PMID: 35377340
  11. Tyrosine kinase inhibition: an approach to drug development.  |  Levitzki, A. and Gazit, A. 1995. Science. 267: 1782-8. PMID: 7892601
  12. Phosphorylation site-specific inhibition of platelet-derived growth factor beta-receptor autophosphorylation by the receptor blocking tyrphostin AG1296.  |  Kovalenko, M., et al. 1997. Biochemistry. 36: 6260-9. PMID: 9174341
  13. Induction of apoptosis and inhibition of small cell lung cancer growth by the quinoxaline tyrphostins.  |  Krystal, GW., et al. 1997. Cancer Res. 57: 2203-8. PMID: 9187122

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AG-1296, 5 mg

sc-200631
5 mg
$121.00

AG-1296, 25 mg

sc-200631A
25 mg
$476.00