1. Cytoskeleton
    Autophagy
  2. Integrin
    Autophagy

Cilengitide (Synonyms: EMD 121974)

Cat. No.: HY-16141 Purity: 98.99%
Handling Instructions

Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, inhibits binding of isolated αvβ3 and αvβ5 to vitronectin with an IC50 value of 4 and 79 nM, respectively.

For research use only. We do not sell to patients.
Cilengitide Chemical Structure

Cilengitide Chemical Structure

CAS No. : 188968-51-6

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10 mM * 1 mL in DMSO USD 171 In-stock
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10 mg USD 224 In-stock
50 mg USD 686 In-stock
100 mg USD 1003 In-stock
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Customer Review

    Cilengitide purchased from MCE. Usage Cited in: PLoS One. 2016 Feb 3;11(2):e0148333.

    Blockade of cellular adhesion of HEK 293 cells at 10 or 30 nM coated recombinant OPN forms with 1μM antagonistic integrin inhibitors. RGES (black bars) is used as a control peptide. Cilengitide (white bars) inhibits the integrins αVβ3, αVβ5, and α5β1. TR-14035 (hatched bars) inhibits the integrins α4β7 and α4β1. Depicted are the means ± SEM of 3 independent experiments. * indicate signif

    Cilengitide purchased from MCE. Usage Cited in: Department of Bioengineering Santa Clara University. 2014.

    Cilengitide Photos: Pictures of migration through alginate with and without Cilengitide after four days. A) The view of the bottom of the untreated well, showing a healthy monolayer of U87s. B) The view of the cells suspended in alginate in the untreated well. A few of the multiple migrated cells within the image are marked with arrows. C) The view of the bottom of the Cilengitide treated well, showing very few, ill-attached U87s. D). The view of cells suspended in alginate in the Cilengitide-tr

    Cilengitide purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2017 Dec 27.

    C2C12 cells are pre-incubated with different concentrations of Cilengitide prior to LPA 20 μg/mL addition and incubation for 3 hours. CTGF levels are analyzed.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, inhibits binding of isolated αvβ3 and αvβ5 to vitronectin with an IC50 value of 4 and 79 nM, respectively.

    IC50 & Target

    IC50: 4 and 79 nM (αvβ3 and αvβ5)[1]

    In Vitro

    Cilengitide (EMD 121974) is the αvβ3 and αvβ5 integrin receptor antagonist. In cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines, Cilengitide inhibits integrin-mediated binding to vitronectin with IC50s of 0.4 and 0.4 μM[1]. In vitro treatment of Cilengitide, at a concentration greater than 1 µM, shows concentration- and time-dependent cytotoxic effects. However, lower doses of Cilengitide monotherapy (0.1 and 0.5 µM) does not elicit the effective death of the both U87MG and U251MG cells. Significant cytotoxic effects are observed in the U87MG cells with the addition of 1 µM Cilengitide in combination with Belotecan monotherapy at concentration of 6.25 nM. Higher concentrations of Cilengitide (5 and 25 µM) does not significantly increase cell death in the U87MG and U251MG compare to a lower concentration of Cilengitide (1 µM)[2].

    In Vivo

    In nude mice bearing M21-L melanoma tumors, Cilengitide dose i.p. at 10, 50, and 250 μg three times per week demonstrated inhibition of tumor growth with a reduction in both tumor volume (55%, 75%, and 89%, respectively) and tumor weight (23%, 38%, and 61%, respectively), when compared to controls[2]. In the rat model studied, the systemic pharmacokinetics of i.p. Cilengitide are not affected by ILP with Cilengitide alone or ILP with Cilengitide plus Melphalan, TNF or both. Systemic Cilengitide levels reach around 20 µg/mL (approximately 35 µM) within 10 min of i.p. administration and continued to rise to approximately 40 µg/mL (approximately 70 µM) in the first hour. Thereafter Cilengitide levels in serum dropped with an elimination half-life of 2.1 hr[3].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.6988 mL 8.4939 mL 16.9877 mL
    5 mM 0.3398 mL 1.6988 mL 3.3975 mL
    10 mM 0.1699 mL 0.8494 mL 1.6988 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    Cilengitide is supplied as an apyrogenic sterile infusion solution in physiological saline. Cilengitide is diluted in saline to a concentration of 1 mM[2].

    The cytotoxicity of the two drugs, Belotecan and Cilengitide, is measured by the Cell Counting Kit-8 (CCK-8). U87MG and U251MG cells are seeded in 96 well plates at a density of 4×103 cells per well to allow for adhesion overnight. After this, the cells are treated with Cilengitide at a concentration of 0, 0.1, 0.5, 1, 5 and 25 µM and Belotecan at a concentration of 0, 6.25, 12.5, 25, 50 and 100 nM. All possible combinations of concentrations are used to assess the combined therapeutic effect of Cilengitide and Belotecan. After 3 days, 10 µL of the CCK-8 solution is added to each well of the plate, and the plate is incubated for 3 hr in the incubator (37°C; 5% CO2). The optical density (OD) of the sample plate is measured at 450 nm in a microplate reader. The viability of tumor cells is assessed by calculating the OD ratio of the specific OD in each sample to that of the control. Each experiment is conducted in quadruplicate. The values are averaged and normalized against the controls to generate dose-response curves[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Cilengitide is prepared in saline.

    Mice[2]
    Male Balb/c-nu mice, at 8 weeks of age, are randomly assigned to four groups: control (n=10), Cilengitide (n=10), Belotecan (n=10) and combination (n=10). Cilengitide is administered intraperitoneally at a dose of 20 mg/kg daily and the Belotecan at a dose of 10 mg/kg every 4 days. The optimal dose is calculated. The control group of animals is injected with saline only. A single dose of the drugs comprised a 3-sec infusion in a volume of 3 mL/kg. The drug treatments began 7 days after the implantation of tumor cells for 16 days. Half of the animals are sacrificed 1 month after the implantation of the tumor cells for tumor volume analysis and the rest of the animals are observed for another 2 months to analyze survival. The death of the animals is defined as a weight reduction of over 25% of the initial weight or an unexpected sudden death beforehand.
    Rats[3]
    Male inbred Brown Norway rats (250 to 300 g) are injected i.p. with 50 mg/kg Cilengitide or saline 2 hr before and 3 hr after Isolated limb perfusion. The Rats are used to investigate the effects of perfusing various combinations of melphalan, TNF and cilengitide with or without the additional i.p. administration of cilengitide before and after the ILP procedure itself. The i.p. administration pre- and post-ILP is intended to optimally saturate available αVβ3 and αVβ5 integrins. Saline is used as a control in both the i.p. and perfusion settings. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    588.66

    Formula

    C₂₇H₄₀N₈O₇

    CAS No.

    188968-51-6

    SMILES

    O=C(NCC(N[[email protected]](C(N[[email protected]](CC1=CC=CC=C1)C(N([[email protected]]2C(C)C)C)=O)=O)CC(O)=O)=O)[[email protected]](CCCNC(N)=N)NC2=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 44 mg/mL; H2O: ≥ 32 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.99%

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    Cilengitide
    Cat. No.:
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