2. Cytoskeleton
  3. Integrin
  4. Cyclo(-RGDfK)

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

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Kundenspezifische Peptidsynthese

CAS. Nr. : 161552-03-0

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Based on 27 publication(s) in Google Scholar

Other Forms of Cyclo(-RGDfK):

Cyclo(-RGDfK) Related Antibodies

Top Publications Citing Use of Products
Bio/Physico-chemical Assay
Cell Migration/Invasion Assay
Cell Proliferation/Viability Assay
WB
In Vivo Efficacy Study

    Cyclo(-RGDfK) purchased from MedChemExpress. Usage Cited in: Mater Today. 2026 Jan 7;92:453-472.

    Cyclo(-RGDfK) (200 μM; 1 h; 37 ℃) significantly reduced intracellular fluorescence intensity, indicating that the constructed LNP-RGD nanoparticles achieved efficient and targeted cellular uptake through RGD–integrin αvβ3 interactions.

    Cyclo(-RGDfK) purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146.  [Abstract]

    Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) pretreatment prevented the S-EMs-induced proliferation of WKY and SHR 24 h after the application of the S-EMs.

    Cyclo(-RGDfK) purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146.  [Abstract]

    Integrin αVβ3 inhibitor Cyclo(-RGDfK) (10 μM) prevented the increased ratios of P-PI3K/PI3K, P-AKT/AKT, and P-FAK/FAK in VSMCs of WKY and SHR that were promoted by S-EMs.

    Cyclo(-RGDfK) purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Aug;14(8):e70146.  [Abstract]

    Cyclo (-RGDfK) (10 mg/kg; i.p.; every 2 d for 10 times) almost abolished vascular remodelling induced by S-EMs in the aorta of WKY mice.

    Cyclo(-RGDfK) purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2021 Jan 7;6(7):2039-2057.  [Abstract]

    The integrin αvβ3 inhibitor Cyclo(-RGDfK) (20 μM; 1 h) significantly inhibited MSC migration.

    Alle Integrin Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

    • Biologische Aktivität

    • Reinheit & Dokumentation

    • Verweise

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    Beschreibung

    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[1][2].

    IC50 & Target

    αvβ3

    0.94 nM (IC50)

    In Vitro

    Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with a IC50 of 0.94 nM[1]. [66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].

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

    Cyclo(-RGDfK) Related Antibodies
    Molekulargewicht

    603.67

    Formel

    C27H41N9O7
    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    Cyclo(Arg-Gly-Asp-{dPhe}-Lys)
    Sequence Shortening

    Cyclo(RGD-{dPhe}-K)
    Versand

    Room temperature in continental US; may vary elsewhere.
    Speicherung

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

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

    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 83.33 mg/mL (138.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 50 mg/mL (82.83 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6565 mL 8.2827 mL 16.5653 mL
    5 mM 0.3313 mL 1.6565 mL 3.3131 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.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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).
    Reinheit & Dokumentation

    Purity: 99.83%

    SDS (396 KB)

    COA (257 KB) HNMR (346 KB) RP-HPLC (256 KB) MS (69 KB) Elemental Analysis Report (115 KB)

    Handling Instructions (2659 KB)
    Verweise

    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 / DMSO 1 mM 1.6565 mL 8.2827 mL 16.5653 mL 41.4134 mL
    5 mM 0.3313 mL 1.6565 mL 3.3131 mL 8.2827 mL
    10 mM 0.1657 mL 0.8283 mL 1.6565 mL 4.1413 mL
    15 mM 0.1104 mL 0.5522 mL 1.1044 mL 2.7609 mL
    20 mM 0.0828 mL 0.4141 mL 0.8283 mL 2.0707 mL
    25 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6565 mL
    30 mM 0.0552 mL 0.2761 mL 0.5522 mL 1.3804 mL
    40 mM 0.0414 mL 0.2071 mL 0.4141 mL 1.0353 mL
    50 mM 0.0331 mL 0.1657 mL 0.3313 mL 0.8283 mL
    60 mM 0.0276 mL 0.1380 mL 0.2761 mL 0.6902 mL
    80 mM 0.0207 mL 0.1035 mL 0.2071 mL 0.5177 mL
    DMSO 100 mM 0.0166 mL 0.0828 mL 0.1657 mL 0.4141 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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    Cyclo(-RGDfK) 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:

    Cyclo(-RGDfK)161552-03-0IntegrinMicrovasculaturecancerαvβ3 integrintumoral cellligandInhibitorinhibitorinhibit

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