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  2. Integrin Autophagy Apoptosis STAT PD-1/PD-L1
  3. Cilengitide

Cilengitide  (Synonyms: EMD 121974)

Cat. No.: HY-16141 Purity: 99.75%
COA Handling Instructions

Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.

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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Customer Review

Based on 44 publication(s) in Google Scholar

Other Forms of Cilengitide:

Top Publications Citing Use of Products

38 Publications Citing Use of MCE Cilengitide

Proliferation Assay
IF
IHC
WB

    Cilengitide purchased from MedChemExpress. Usage Cited in: Cell Adh Migr. 2019 Jan 21:1-12.   [Abstract]

    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.

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

    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 MedChemExpress. Usage Cited in: J Transl Med. 2018 Dec 12;16(1):352.  [Abstract]

    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 MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2018 Apr 1;314(4):C415-C427.  [Abstract]

    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 MedChemExpress. Usage Cited in: PLoS One. 2016 Feb 3;11(2):e0148333.  [Abstract]

    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 MedChemExpress. 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
    • Biological Activity

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    Description

    Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers[1][2][3].

    IC50 & Target[1][2][3]

    αvβ3

    4 nM (IC50, αvβ3-Vitronectin interaction[2])

    αvβ5

    79 nM (IC50, αvβ5-Vitronectin interaction[2])

    αvβ3

    0.61 nM (IC50, [1])

    αvβ5

    8.4 nM (IC50, [1])

    α5β1

    14.9 nM (IC50, [1])

    STAT3

     

    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[2].
    Cilengitide inhibits integrin-mediated binding to Vitronectin with IC50s of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines[2].
    Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC50 of 2 μM[2].
    Cilengitide (0-1 mg/mL; 24-72 h) inhibits cell viability of melanoma cells in vitro and (5 μg/mL; 12 h) induces B16 and A375 cells apoptosis[3].
    Cilengitide (5 μg/mL, 10 μg/mL; 2 weeks) inhibits colony formation of B16 and A375 cells[3].
    Cilengitide (0-20 μg/mL; 12 h) inhibits STAT3 phosphorylation to decrease the expression of PD-L1[3].

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

    Western Blot Analysis[3]

    Cell Line: B16 and A375 cells
    Concentration: 0, 5, 10, and 20 μg/mL
    Incubation Time: 12 hours
    Result: Suppressed PD-L1 expression and STAT3 phosphorylation at concentrations greater than 5 µg/mL.

    Apoptosis Analysis[3]

    Cell Line: B16 and A375 cells
    Concentration: 5 μg/mL
    Incubation Time: 12 hours
    Result: Resulted apoptosis rates in B16 and A375 cells of 15.27% and 14.89%, respectively.
    In Vivo

    Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice[2].
    Cilengitide (50 mg/kg; i.p.; daily) enhances the function of CD8+ T cells and promotes anti-PD1 efficacy with Anti-PD1 monoclonal antibody in B16 murine melanoma model[3].

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

    Animal Model: Nude mice bearing M21-L melanoma tumors[2]
    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.
    Animal Model: Female C57BL/6 mice (6-8 weeks old) with B16 cells s.c.[3]
    Dosage: 50 mg/kg; with or without 10 mg/kg Anti-PD1 monoclonal antibody or isotype control i.p. every 3 days;
    Administration: Intraperitoneal injection; daily
    Result: Downregulated the expression of PD-L1 via STAT3 pathway and decreased the expression of PD-L1.
    Clinical Trial
    Molecular Weight

    588.66

    Formula

    C27H40N8O7

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(NCC(N[C@H](C(N[C@H](CC1=CC=CC=C1)C(N([C@H]2C(C)C)C)=O)=O)CC(O)=O)=O)[C@H](CCCNC(N)=N)NC2=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    H2O : 100 mg/mL (169.88 mM; Need ultrasonic)

    DMSO : ≥ 44 mg/mL (74.75 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.
    In Vivo:
    • 1.

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (169.88 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.80%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Cilengitide
    Cat. No.:
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