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  3. Cilengitide

Cilengitide  (Synonyms: EMD 121974)

製品番号: HY-16141 純度: 99.91%
COA 取扱説明書 Technical Support

Cilengitide (EMD 121974) is a BBB-permeable 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.

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CAS 番号 : 188968-51-6

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10 mM * 1 mL in DMSO
ready for reconstitution
USD 171 在庫あり
Solution
10 mM * 1 mL in DMSO USD 171 在庫あり
Solid
5 mg $132 在庫あり
10 mg $224 在庫あり
25 mg $380 在庫あり
50 mg $530 在庫あり
100 mg $740 在庫あり
200 mg $1166 在庫あり
500 mg $2333 在庫あり
1 g $3500 在庫あり
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カスタマーレビュー

Based on 70 publication(s) in Google Scholar

Other Forms of Cilengitide:

Top Publications Citing Use of Products

顧客検証

Cell Proliferation/Viability Assay
IF
IHC
WB

    Cilengitide purchased from MedChemExpress. Usage Cited in: Cell Adh Migr. 2019 Dec;13(1):152-163.  [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 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: 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: 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: Santa Clara University. 2014 Jun 12.

    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
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Cilengitide (EMD 121974) is a BBB-permeable 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

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    0.54 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    M21 IC50
    0.4 1
    Compound: c[RGDf(Me)V]; Cilengitide
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    [PMID: 26753814]
    CHO IC50
    0.54 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    CHO IC50
    15.4 1
    Compound: Cilengitide
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    HEK-293T IC50
    0.51 1
    Compound: c(RGDfV)
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    [PMID: 24095096]
    CHO IC50
    15.4 1
    Compound: Cilengitide
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    CHO IC50
    8 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    CHO IC50
    8 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    CHO IC50
    0.54 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    HEK-293T IC50
    0.51 1
    Compound: c(RGDfV)
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    [PMID: 24095096]
    CHO IC50
    8 1
    Compound: Cilengitide
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    M21 IC50
    0.4 1
    Compound: c[RGDf(Me)V]; Cilengitide
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    [PMID: 26753814]
    CHO IC50
    15.4 1
    Compound: Cilengitide
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay
    [PMID: 32094009]
    HEK-293T IC50
    0.51 1
    Compound: c(RGDfV)
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay
    [PMID: 24095096]
    M21 IC50
    0.4 3
    Compound: 2
    Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6
    Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6
    [PMID: 11855984]
    M21 IC50
    0.4 1
    Compound: c[RGDf(Me)V]; Cilengitide
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2
    [PMID: 26753814]
    M21 IC50
    0.4 3
    Compound: 2
    Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6
    Inhibition of integrin alpha-v/beta-3 mediated M21 cell adhesion to vitronectin with monoclonal antibody P1F6
    [PMID: 11855984]
    体外実験

    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.
    体内実験

    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.
    臨床実験
    分子量

    588.66

    分子式

    C27H40N8O7

    CAS 番号
    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 44 mg/mL (74.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 35 mg/mL (59.46 mM; Need ultrasonic)

    *"≥" 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
    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * 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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    一般には略語で表示されます:C1V1 = C2V2

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

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    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).
    純度とドキュメンテーション

    純度: 99.91%

    参考文献

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.6988 mL 8.4939 mL 16.9877 mL 42.4693 mL
    5 mM 0.3398 mL 1.6988 mL 3.3975 mL 8.4939 mL
    10 mM 0.1699 mL 0.8494 mL 1.6988 mL 4.2469 mL
    15 mM 0.1133 mL 0.5663 mL 1.1325 mL 2.8313 mL
    20 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1235 mL
    25 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
    30 mM 0.0566 mL 0.2831 mL 0.5663 mL 1.4156 mL
    40 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
    50 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
    DMSO 60 mM 0.0283 mL 0.1416 mL 0.2831 mL 0.7078 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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Cilengitide
    製品番号:
    HY-16141
    数量:
    MCE 日本正規代理店: