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: 西仑吉肽; EMD 121974)

目录号: HY-16141 纯度: 99.75%
COA 产品使用指南

摩尔计算器

Cilengitide (EMD 121974) 是一种强效的整合素拮抗剂，IC50 分别为 0.61 nM (ανβ3)，8.4 nM (ανβ5) 和 14.9 nM (α5β1)。Cilengitide 抑制 ανβ3 和 ανβ5 与玻连蛋白结合，IC50 值分别为 4 和 79 nM。Cilengitide 能够抑制 TGF-β/Smad 信号通路，调节 PD-L1 表达。Cilengitide 诱导凋亡 (apoptosis)，在对胶质母细胞瘤和其他癌症的研究中也显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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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1590
In-stock
5 mg ￥1220
In-stock
10 mg ￥1730
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Cilengitide:

Cilengitide 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 38 篇科研文献

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 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: 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: 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

    查看 Integrin 亚型特异性产品:

    查看所有亚型
    αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

    查看 STAT 亚型特异性产品:

    查看所有亚型
    STAT3 STAT5 STAT6 STAT1

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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

     

    体外研究
    (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.

    Cilengitide 相关抗体:

    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 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    西仑吉肽
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 100 mg/mL (169.88 mM; 超声助溶)

    DMSO 中的溶解度 : ≥ 44 mg/mL (74.75 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 100 mg/mL (169.88 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.80%

    COA (198 KB) HNMR (312 KB) LCMS (86 KB) 元素分析报告 (215 KB)

    产品使用指南 (1538 KB)
    参考文献

    Cilengitide 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 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
    H2O 80 mM 0.0212 mL 0.1062 mL 0.2123 mL 0.5309 mL
    100 mM 0.0170 mL 0.0849 mL 0.1699 mL 0.4247 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Cilengitide188968-51-6EMD 121974西仑吉肽EMD121974EMD-121974IntegrinAutophagyApoptosisSTATPD-1/PD-L1PD-1/Programmed death-ligand 1integrinsανβ3ανβ5VitronectinInhibitorinhibitorinhibit

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