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  3. Cilengitide TFA

Cilengitide TFA (Synonyms: EMD 121974 TFA)

Cat. No.: HY-16143
Handling Instructions

Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.

For research use only. We do not sell to patients.

Cilengitide TFA Chemical Structure

Cilengitide TFA Chemical Structure

CAS No. : 199807-35-7

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Top Publications Citing Use of Products

    Cilengitide TFA 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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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.
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    Description

    Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.

    IC50 & Target

    IC50: 4/79 nM (αvβ3vβ5)[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 [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 demonstrate 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 drop with an elimination half-life of 2.1 hr[3].

    Molecular Weight

    702.68

    Formula

    C₂₉H₄₁F₃N₈O₉

    CAS No.

    199807-35-7

    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.FC(F)(C(O)=O)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Cell Assay
    [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)[2].

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

    Animal Administration
    [2][3]

    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 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[2].

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

    References
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    Keywords:

    CilengitideEMD 121974EMD121974EMD-121974IntegrinAutophagyInhibitorinhibitorinhibit

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