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Cilengitide
Cat No.
CEI-1282
Description
Cilengitide is a small-molecule inhibitor of integrins with IC50 values of 2.3 nM and 37 nM for αvβ3 and αvβ5, respectively.
Product Overview
Cilengitide is a cyclic RGD pentapeptide [Arg-Gly-Asp-DPhe-(NMeVal)], and a potent α vβ 3 and α vβ 5 integrin inhibitor to block integrin-mediated adhesion and migration. It can directly bind α vβ 3 integrin. Its IC50 is 250 nM as an α vβ 3 inhibitor. Integrins are named for a family including 24 transmembrane heterodimer receptors that are composed of paired alpha and beta chains. These receptors can integrate extracellular and intracellular activities. Consequently, they can regulate tumor angiogenesis, migration and invasion. When treated with cilengitide, a significant dose-dependent reduction of proliferation was noted (p<0.0002) in cell lines developed through 28 d of expansion and hence 14 d of differentiation culture of CD133+ stem cells (with VEGF, SCGF and FLT3L, to prepare CD133+ EPCs, i. e. endothelial progenitor cells). When treated with cilengitide after withdrawal of FLT3L and SCGF, a dose-dependent decrease of adherent cells was noted in EPCs after 7 and 14 days (p<0.03). Compared with which on EPC proliferation, the inhibitory effect of cilengitide on endothelial cell attachment was more pronounced. Therapy with cilengitide intraperitoneally 5 times per week between days 1 and 30 after injection of MDA-MB-231 cells (105), volumes of osteolytic lesions(OL) and soft tissue components(SC) were significantly reduced on days 30 and 35 in rats, compared with untreated nude rats (p<0.05)
CAS No.
188968-51-6
Molecular Weight
588.66
Purity
0.993
Storage
Store at-20°C
Targets
αvβ3; αvβ5; α5β1
IC50
2.3 nM; 37 nM
Molecular Formula
C27H40N8O7
Chemical Name
2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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