2. Cytoskeleton Autophagy
  3. Integrin Autophagy
  4. Cilengitide TFA

Cilengitide TFA  (Synonyms: EMD 121974 TFA)

Cat. No.: HY-16143 Purity: 99.92%
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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 139 In-stock
Solution
10 mM * 1 mL in Water USD 139 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 290 In-stock
50 mg USD 450 In-stock
100 mg USD 700 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 49 publication(s) in Google Scholar

Other Forms of Cilengitide TFA:

Cilengitide TFA Related Antibodies

Top Publications Citing Use of Products

43 Publications Citing Use of MCE Cilengitide TFA

Proliferation Assay
IF
IHC
WB

    Cilengitide TFA 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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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

    View All Integrin Isoform Specific Products:

    View All Isoforms
    αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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 (αvβ3/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 [2].

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

    Cilengitide TFA Related Antibodies
    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].

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

    702.68

    Formula

    C29H41F3N8O9
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (71.16 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4231 mL 7.1156 mL 14.2312 mL
    5 mM 0.2846 mL 1.4231 mL 2.8462 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 16.67 mg/mL (23.72 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.4231 mL 7.1156 mL 14.2312 mL 35.5781 mL
    5 mM 0.2846 mL 1.4231 mL 2.8462 mL 7.1156 mL
    10 mM 0.1423 mL 0.7116 mL 1.4231 mL 3.5578 mL
    15 mM 0.0949 mL 0.4744 mL 0.9487 mL 2.3719 mL
    20 mM 0.0712 mL 0.3558 mL 0.7116 mL 1.7789 mL
    25 mM 0.0569 mL 0.2846 mL 0.5692 mL 1.4231 mL
    30 mM 0.0474 mL 0.2372 mL 0.4744 mL 1.1859 mL
    40 mM 0.0356 mL 0.1779 mL 0.3558 mL 0.8895 mL
    50 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7116 mL
    60 mM 0.0237 mL 0.1186 mL 0.2372 mL 0.5930 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cilengitide TFA Related Classifications

    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.

    Keywords:

    Cilengitide199807-35-7EMD 121974EMD121974EMD-121974IntegrinAutophagyInhibitorinhibitorinhibit

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