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Description: Potent and selective inhibitor of integrins αvβ3 and αvβ5
Alternative Names: EMD121974
Purity: ≥95% (HPLC)
Citations (6)
Literature (2)

Biological Activity for Cilengitide

Cilengitide is a potent and selective inhibitor of integrins αvβ3 and αvβ5 (IC50 values are 4.1 and 70 nM, respectively). Exhibits ~10-fold selectivity over gpIIb/IIIa. Increases endothelial monolayer permeability. Also exhibits antiangiogenic activity.

Technical Data for Cilengitide

M. Wt 588.66
Formula C27H40N8O7
Sequence RGDFV

(Modifications: Phe-4 = D-Phe, Val-5 = Me-Val, Cyclized)

Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 188968-51-6
PubChem ID 176873
Smiles CC(C)[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Cilengitide

Solubility Soluble to 10 mg/ml in water

Product Datasheets for Cilengitide

Certificate of Analysis / Product Datasheet
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References for Cilengitide

References are publications that support the biological activity of the product.

Alghisi et al (2009) The integrin antagonist cilengitide activates αvβ3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells. PLoS One 4 e4449 PMID: 19212436

Monnier et al (2008) CYR61 and αvβ5 integrin cooperate to promote invasion and metastasis of tumors growing in preirradiated stroma. Cancer Res. 68 7323 PMID: 18794119

If you know of a relevant reference for Cilengitide, please let us know.

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Keywords: Cilengitide, Cilengitide supplier, Potent, selective, inhibitors, inhibits, integrin, αvβ3, αvβ5, alphavbeta3, alphavbeta5, EMD121974, Integrins, Cell, Adhesion, Molecules, 5870, Tocris Bioscience

6 Citations for Cilengitide

Citations are publications that use Tocris products. Selected citations for Cilengitide include:

Filla et al (2019) Activation of αvβ3 Integrin Alters Fibronectin Fibril Formation in Human Trabecular Meshwork Cells in a ROCK-Independent Manner. Invest Ophthalmol Vis Sci 60 3897 PMID: 31529121

Elazer R et al (2019) Subendothelial matrix components influence endothelial cell apoptosis in vitro. Am J Physiol Cell Physiol 316 C210-C222 PMID: 30566394

Albarrán-Juárez et al (2018) Piezo1 and Gq/G11 promote endothelial inflammation depending on flow pattern and integrin activation. J Exp Med 215 2655 PMID: 30194266

Adriano et al (2022) G protein-coupled receptor kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by chemokine receptor CXCR4. J Biol Chem 298 102351 PMID: 35940305

Do you know of a great paper that uses Cilengitide from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Enabling Research By Provision of Chemical Tools Poster

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.