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  2. Cytoskeleton Autophagy Apoptosis Stem Cell/Wnt JAK/STAT Signaling Immunology/Inflammation
  3. Integrin Autophagy Apoptosis STAT PD-1/PD-L1
  4. Cilengitide

Cilengitide  (Synonyms: 西侖吉肽; EMD 121974)

目錄號(hào): HY-16141 純度: 99.80%
COA 產(chǎn)品使用指南 技術(shù)支持

Cilengitide (EMD 121974) 是一種強(qiáng)效的整合素拮抗劑，IC50 分別為 0.61 nM (ανβ3)，8.4 nM (ανβ5) 和 14.9 nM (α5β1)。Cilengitide 抑制 ανβ3 和 ανβ5 與玻連蛋白結(jié)合，IC50 值分別為 4 和 79 nM。Cilengitide 能夠抑制 TGF-β/Smad 信號(hào)通路，調(diào)節(jié) PD-L1 表達(dá)。Cilengitide 誘導(dǎo)凋亡 (apoptosis)，在對(duì)膠質(zhì)母細(xì)胞瘤和其他癌癥的研究中也顯示出抗血管生成的作用。

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Cilengitide Chemical Structure

Cilengitide Chemical Structure

CAS No. : 188968-51-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1580
In-stock
1 mg ￥491
In-stock
5 mg ￥1220
In-stock
10 mg ￥1730
In-stock
25 mg ￥2980
In-stock
50 mg ￥4488
In-stock
100 mg 現(xiàn)貨 詢(xún)價(jià)
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of Cilengitide:

MCE 顧客使用本產(chǎn)品發(fā)表的 43 篇科研文獻(xiàn)

Proliferation Assay
IF
WB
IHC

    Cilengitide purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 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

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    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

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    0.54 nM
    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 nM
    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 nM
    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]
    HEK-293T IC50
    0.51 nM
    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 nM
    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]
    體外研究
    (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].

    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.
    體內(nèi)研究
    (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].

    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
    分子量

    588.66

    Formula

    C27H40N8O7
    CAS 號(hào)
    性狀

    固體

    顏色

    White to light yellow

    中文名稱(chēng)

    西侖吉肽
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 44 mg/mL (74.75 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    H2O 中的溶解度 : 40 mg/mL (67.95 mM; adjust pH to 1 with 1 M HCL)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： PBS

      Solubility: 100 mg/mL (169.88 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.80%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 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
    60 mM 0.0283 mL 0.1416 mL 0.2831 mL 0.7078 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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    產(chǎn)品名稱(chēng)：
    Cilengitide
    目錄號(hào)：
    HY-16141
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