Cayman Chemical | SU 11652 | Description (CAS 326914-10-7)

13577 SU 11652

(CAS 326914-10-7)

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• See more Inhibitors; Angiogenesis; Apoptosis; Cancer; Cell Cycle

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Several growth factor receptors (GFRs) act as receptor tyrosine kinases (RTKs). Ligand binding triggers autophosphorylation of tyrosine residues on intracellular portions of the receptor, potentiating signaling to cause the growth response. SU 11652 is a potent, cell-permeable, and ATP-competitive inhibitor of the tyrosine kinase activity of several GFRs, including platelet-derived GFR (PDGFR-β; IC₅₀ = 3 nM), vascular endothelial GFR (VEGFR-2; IC₅₀ = 27 nM), and fibroblast GFR (FGFR1; IC₅₀ = 170 nM), but not epidermal GFR (EGFR; IC₅₀ > 20 μM).¹ SU 11652 also potently inhibits wild-type Kit in mast cells (IC₅₀ = 50 nM) and stops cell cycling while inducing apoptosis in cells expressing constitutively-active Kit mutants.² Furthermore SU 11652 reduces angiogenesis induced by estrogen in mice.³

1 Sun, L., Liang, C., Shirazian, S., et al. Discovery of 5-[5-Fluoro-2-oxo-1,2-dihydroindol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem 46 1116-1119 (2003).

2 Liao, A.T., Chien, M.B., Shenoy, N., et al. Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors. Blood 100(2) 585-593 (2002).

3 Heryanto, B., Lipson, K.E., Rogers, P.A.W. Effect of angiogenesis inhibitors on oestrogen-mediated endometrial endothelial cell proliferation in the ovariectomized mouse. Reproduction 125 337-346 (2003).

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Pricing updated 2010-03-20.
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