AG 1296

Similar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC₅₀ = 1.0 µM) and β-receptors (IC₅₀ = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60^c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC₅₀ of 300 nM and ~1 µM, respectively.

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Tse, KF., et al. 2002. Leukemia16, 2027.
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Strutz, F., et al. 2001. Kidney Int.59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.

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