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Cilengitide Integrin inhibitor for αvβ3 and αvβ5

Catalog No.A8660
Size Price Stock Qty
10mM (in 1mL DMSO)
$170.00
In stock
5mg
$128.00
In stock
10mg
$183.00
In stock
25mg
$323.00
In stock
50mg
$560.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Biological Activity

Description Cilengitide is a small-molecule inhibitor of integrins with IC50 values of 2.3 nM and 37 nM for αvβ3 and αvβ5, respectively.
Targets αvβ3 αvβ5 α5β1      
IC50 2.3 nM 37 nM        

Protocol

Cell experiment [1]:

Cell lines

meningioma lines (Ben-Men1, IOMM-Lee, HBL-52)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

24 h; 100 μM/mL

Applications

Cilengitide(1, 10, and 100 μM/mL) was added to IOMM-Lee,HBL52, and Ben-Men1 cultures. Morphologic changes were monitored over 24 hours. In all three meningioma lines, cells strated to round up and detach from the flask in a concentration-dependent manner, showing that cilengitide decreases cell adhesion. Quantification of cell viability after 24 hours, cilengitide treatment showed in all three cell lines a highly significant dose-dependent but rather mild decline of viable cells.

Animal experiment [1]:

Animal models

8- to 10-week-old Swiss Nude mice

Dosage form

75 mg/kg; intraperitoneal injection

Applications

We intended to test a daily dosage of cilengitide (75 mg/kg) as a monotherapy or combined with irradiation in the orthotopic mouse model. A significant reduction of tongue-like brain invasion (P≤0.01) could be observed in tumors of mice treated with either cilengitide alone (35% decrease) or with cilengitide and irradiation (35.5% decrease).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wilisch-Neumann A, Kliese N, Pachow D, et al. The integrin inhibitor cilengitide affects meningioma cell motility and invasion[J]. Clinical Cancer Research, 2013, 19(19): 5402-5412.

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Chemical Properties

Cas No. 188968-51-6 SDF Download SDF
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
Canonical SMILES CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N
Formula C27H40N8O7 M.Wt 588.66
Solubility >29.4mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Cilengitide is a cyclic RGD pentapeptide [Arg-Gly-Asp-DPhe-(NMeVal)], and a potent αvβ3 and αvβ5 integrin inhibitor to block integrin-mediated adhesion and migration. It can directly bind αvβ3 integrin. Its IC50 is 250 nM as an αvβ3 inhibitor [1] [2] [3] [4].
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 [2].
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 [3].
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) [5].
References:
[1]. Carlos Mas-Moruno, Florian Rechenmacher and Horst Kessler. Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation. Anti-Cancer Agents in Medicinal Chemistry, 2010, 10(10): 753-768.
[2]. David A Reardon, L Burt Nabors, Roger Stupp, et al. Cilengitide: an integrin-targeting arginine-glycine-aspartic acid peptide with promising activity for glioblastoma multiforme. Expert Opin Investig Drugs, 2008, 17(8):1225-1235.
[3]. Sonja Loges, Martin Butzal, Jasmin Otten, et al. Cilengitide inhibits proliferation and differentiation of human endothelial progenitor cells in vitro. Biochemical and Biophysical Research Communications, 2007, 357: 1016-1020.
[4]. Despoina Sykoutri, Nisha Geetha, Silvia Hayer, et al. αvβ3 Integrin Inhibition with Cilengitide both Prevents and Treats Collagen Induced Arthritis. Ann Rheum Dis, 2013, 72(Suppl 1):A1-A88.
[5]. Maren Bretschi, Maximilian Merz, Dorde Komljenovic, et al. Cilengitide inhibits metastatic bone colonization in a nude rat model. Oncology Reports, 2011, 26:843-851.