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

Cilengitide TFA  (Synonyms: EMD 121974 TFA)

目录号: HY-16143 纯度: 96.96%
COA 产品使用指南

Cilengitide 是有效的,选择性的 αvβ3 和 αvβ5 受体整合素抑制剂,IC50 分别为 4 nM 和 79 nM。

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Cilengitide TFA Chemical Structure

Cilengitide TFA Chemical Structure

CAS No. : 199807-35-7

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥1390
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5 mg ¥900
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10 mg ¥1500
In-stock
25 mg ¥2900
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50 mg ¥4500
In-stock
100 mg ¥7000
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Customer Review

Other Forms of Cilengitide TFA:

MCE 顾客使用本产品发表的 38 篇科研文献

Proliferation Assay
IF
WB
IHC

    Cilengitide TFA 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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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 (αvβ3vβ5)[1].

    体外研究
    (In Vitro)

    Cilengitide (EMD 121974) 是 αvβ3 和 αvβ5 整合素受体拮抗剂。在评估人黑色素瘤 M21 或 UCLA-P3 人肺癌细胞系的细胞粘附研究中,Cilengitide 抑制整合素介导的与玻连蛋白的结合,IC50 分别为 0.4 和 0.4 μM[1]。体外处理浓度大于 1 μM 的 Cilengitide,表现出浓度和时间依赖性细胞毒性作用[2]

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

    体内研究
    (In Vivo)

    在携带 M21-L 黑色素瘤肿瘤的裸鼠中,每周 3 次 10、50 和 250 μg 的西仑吉肽腹腔注射;剂量显示抑制肿瘤生长并同时减少肿瘤体积 (分别为 55%、75% 和 89%) 和肿瘤重量 (分别为 23%、38% 和 61%)[2]。在所研究的大鼠模型中,西仑吉肽腹腔注射;的全身药代动力学不受 ILP 单独使用西仑吉肽或 ILP 与西仑吉肽加美法仑、TNF 或两者的影响。西仑吉肽的全身水平在腹膜内给药 10 分钟内达到约 20 μg/mL (约 35 μM),并在第一个小时内继续上升至约 40 μg/mL (约 70 μM)。此后,血清中的 Cilengitide 水平下降,消除半衰期为 2.1 小时[3]

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

    Clinical Trial
    分子量

    702.68

    Formula

    C29H41F3N8O9

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, sealed storage, away from moisture

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

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : ≥ 100 mg/mL (142.31 mM)

    * "≥" 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 1.4231 mL 7.1156 mL 14.2312 mL
    5 mM 0.2846 mL 1.4231 mL 2.8462 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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: 16.67 mg/mL (23.72 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

    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
    参考文献
    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.

    参考文献

    Cilengitide TFA 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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
    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
    80 mM 0.0178 mL 0.0889 mL 0.1779 mL 0.4447 mL
    100 mM 0.0142 mL 0.0712 mL 0.1423 mL 0.3558 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.

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    产品名称:
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    目录号:
    HY-16143
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