1. Cytoskeleton
    Autophagy
  2. Integrin
    Autophagy
  3. Cilengitide

Cilengitide (Synonyms: EMD 121974)

Cat. No.: HY-16141 Purity: 99.32%
Handling Instructions

Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 171 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 224 In-stock
Estimated Time of Arrival: December 31
50 mg USD 686 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1003 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of Cilengitide:

Top Publications Citing Use of Products

    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. Jun 12, 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. 2018 Apr 1;314(4):C415-C427.

    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.

    Cilengitide purchased from MCE. Usage Cited in: J Transl Med. 2018 Dec 12;16(1):352.

    Representative images of immunofluorescence performed for α-SMA on WKY- and SHR-CF in the treatment of TGF-β1, cilengitide or both.

    Cilengitide purchased from MCE. Usage Cited in: J Transl Med. 2018 Dec 12;16(1):352.

    Representative Western blot images of ανβ5 and collagen I protein expression in WKY- and SHR-CF cultured on substrates with two different stiffness (high and low) and contemporary treated with 5 ng/ml TGF-β1, TGF-β1 + 0.5 μM cilengitide, or cilengitide.

    Cilengitide purchased from MCE. Usage Cited in: Cell Adh Migr. 2019 Jan 21:1-12. 

    HepG2 cells are loaded with FSS at 1 dyn/cm2 for 0.5 h, with or without treatment of 0.5 μM Cli for 6 h prior to FSS application. Lysates are probed with antibodies as indicated.
    • Biological Activity

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    Description

    Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to Vitronectin with an IC50 value of 4 and 79 nM, respectively [1].

    IC50 & Target[1]

    αvβ3

    4 nM (IC50, Binds to Vitronectin)

    αvβ5

    79 nM (IC50, Binds to Vitronectin)

    In Vitro

    Cilengitide is a cyclized RGD (Arg-Gly-Asp motif)-containing pentapeptide. Cilengitide blocks integrin ανβ3- and ανβ5-mediated endothelial cell attachment and migration[1].
    Cilengitide inhibits integrin-mediated binding to Vitronectin with IC50's of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines [1].
    Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC50 of 2 μM [1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice [1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Nude mice bearing M21-L melanoma tumors[1]
    Dosage: 10, 50, and 250 μg
    Administration: Dosed i.p. three times per week
    Result: 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.
    Clinical Trial
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 44 mg/mL (74.75 mM)

    H2O : ≥ 32 mg/mL (54.36 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    References

    Purity: 99.32%

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    Keywords:

    CilengitideEMD 121974EMD121974EMD-121974IntegrinAutophagyintegrinsανβ3ανβ5VitronectinInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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