Cilengitide

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Cat.No. 5870 - Cilengitide | cyclo(Arg-Gly-Asp-D-Phe-(NMe)-Val) | CAS No. 188968-51-6
Description: Potent and selective inhibitor of integrins αvβ3 and αvβ5
Alternative Names: EMD121974
Datasheet
Citations
Literature

Biological Activity

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

M. Wt 588.66
Formula C27H40N8O7
Sequence RGDFV

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

Storage Store at -20°C
CAS Number 188968-51-6
PubChem ID 176873
InChI Key AMLYAMJWYAIXIA-VWNVYAMZSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 10 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 588.66. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.7 mL 8.49 mL 16.99 mL
5 mM 0.34 mL 1.7 mL 3.4 mL
10 mM 0.17 mL 0.85 mL 1.7 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References

References are publications that support the products' biological activity.

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


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

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Literature in this Area

Immunology

Immunology Product Listing

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  • Chemotaxis
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