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

Cilengitide TFA  (Synonyms: EMD 121974 TFA)

目錄號(hào): HY-16143 純度: 99.92%
COA 產(chǎn)品使用指南

Cilengitide 是有效的,選擇性的 αvβ3 和 αvβ5 受體整合素抑制劑,IC50 分別為 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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10 mM * 1 mL in Water ¥1390
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10 mg ¥1500
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25 mg ¥2900
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Customer Review

Other Forms of Cilengitide TFA:

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 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 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: 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: 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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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].

    體外研究
    (In Vitro)

    Cilengitide (EMD 121974) 是 αvβ3 和 αvβ5 整合素受體拮抗劑。在評(píng)估人黑色素瘤 M21 或 UCLA-P3 人肺癌細(xì)胞系的細(xì)胞粘附研究中,Cilengitide 抑制整合素介導(dǎo)的與玻連蛋白的結(jié)合,IC50 分別為 0.4 和 0.4 μM[1]。體外處理濃度大于 1 μM 的 Cilengitide,表現(xiàn)出濃度和時(shí)間依賴性細(xì)胞毒性作用[2]。

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

    體內(nèi)研究
    (In Vivo)

    在攜帶 M21-L 黑色素瘤腫瘤的裸鼠中,每周 3 次 10、50 和 250 μg 的西侖吉肽腹腔注射;劑量顯示抑制腫瘤生長(zhǎng)并同時(shí)減少腫瘤體積 (分別為 55%、75% 和 89%) 和腫瘤重量 (分別為 23%、38% 和 61%)[2]。在所研究的大鼠模型中,西侖吉肽腹腔注射;的全身藥代動(dòng)力學(xué)不受 ILP 單獨(dú)使用西侖吉肽或 ILP 與西侖吉肽加美法侖、TNF 或兩者的影響。西侖吉肽的全身水平在腹膜內(nèi)給藥 10 分鐘內(nèi)達(dá)到約 20 μg/mL (約 35 μM),并在第一個(gè)小時(shí)內(nèi)繼續(xù)上升至約 40 μg/mL (約 70 μM)。此后,血清中的 Cilengitide 水平下降,消除半衰期為 2.1 小時(shí)[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 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    H2O 中的溶解度 : 50 mg/mL (71.16 mM; 超聲助溶)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑: PBS

      Solubility: 16.67 mg/mL (23.72 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

    由于實(shí)驗(yàn)過程有損耗,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
    參考文獻(xiàn)
    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.

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(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 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

    * 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 的濾膜過濾除菌后使用。

    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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    產(chǎn)品名稱:
    Cilengitide TFA
    目錄號(hào):
    HY-16143
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