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SU 11652, 1 mg  

SU 11652, 1 mg

5-[(Z)-(5-chloro-2-oxo-1H-indol-3-ylidene)methyl]-N-[2- (diethylamino) ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide

Synonyms: SU 11652, SU-11652, SU11652
potent ATP competitive inhibitor of VEGFR2, PDGFRβ and FGFR1

More details

PKI-SU11652-001

Availability: within 3 days

295,00 €

Background: SU11652 is an indolinone-based compound acting as competitive inhibitor with respect to ATP at the catalytic site of several RTKs (IC50 of 27 nM, 3 nM, and 170 nM for VEGFR2, PDGFRβ and FGFR1). The cell-permeable compound negatively affects Kit phosphorylation in mastocytoma cell lines resulting in cell cycle arrest and apoptosis (IC50 of 10-500 nM). SU11652 reduces endothelial cell proliferation upon oestrogen stimulation in ovariectomized mouse. Recent studies revealed that SU 11652 displays antiproliferative and pro-apoptotic properties in tumor cells and effects also kinase activity of serine/threonine protein kinases like NEK2 (IC50 of 8 µM).

Formula:  C22H27ClN4O2
Molecular Weight:  414.9 g/mol
Purity:  >98%
Appearance:  Orange powder
Solubility:  soluble in DMSO (>25 mg/ml)
CAS No. 326914-10-7

Product specific literature references:

Liao AT, Chien MB, Shenoy N, Mendel DB, McMahon G, Cherrington JM, London CA. (2002) “Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors. Blood.15; 100(2):585-93.

Rellos P, Ivins FJ, Baxter JE, Pike A, Nott TJ, Parkinson DM, Das S, Howell S, Fedorov O, Shen QY, Fry AM, Knapp S, Smerdon SJ.(2007) “Structure and regulation of the human Nek2 centrosomal kinase.” J Biol Chem. 2007 Mar 2;282(9):6833-42. Epub 2006 Dec 31.

Heryanto B, Lipson KE, Rogers PA.(2003) “Effect of angiogenesis inhibitors on oestrogen-mediated endometrial endothelial cell proliferation in the ovariectomized mouse.” Reproduction.125(3):337-46.

Sun L, Liang C, Shirazian S, Zhou Y, Miller T, Cui J, Fukuda JY, Chu JY, Nematalla A, Wang X, Chen H, Sistla A, Luu TC, Tang F, Wei J, Tang C. (2003)“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. 27;46(7):1116-9.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

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