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  1. Apoptosis Autophagy
  2. Survivin Autophagy
  3. Sepantronium bromide

Sepantronium bromide  (Synonyms: YM-155)

目錄號(hào): HY-10194 純度: 99.36%
COA 產(chǎn)品使用指南 技術(shù)支持

Sepantronium bromide (YM-155) 是一種 survivin 抑制劑,其 IC50 為 0.54 nM。

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Sepantronium bromide Chemical Structure

Sepantronium bromide Chemical Structure

CAS No. : 781661-94-7

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Customer Review

Other Forms of Sepantronium bromide:

    Sepantronium bromide purchased from MCE. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617.   [Abstract]

    A2780 CSLCs are treated in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).

    Sepantronium bromide purchased from MCE. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353.  [Abstract]

    Influences of YM155, a chemical inhibitor of survivin on ABT-737-induced apoptosis are analyzed by western blot.
    • 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

    Sepantronium bromide (YM-155) is a survivin inhibitor with an IC50 of 0.54 nM[1].

    IC50 & Target

    IC50: 0.54 nM (Survivin)[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    DU-145 EC50
    13.8 nM
    Compound: YM155
    Cytotoxicity against human DU145 cells by MTT assay
    Cytotoxicity against human DU145 cells by MTT assay
    [PMID: 28774426]
    MDA-MB-435 IC50
    > 1 μM
    Compound: YM-155
    Antiproliferative activity against human MDA-MB-435/LCC6MDR cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
    Antiproliferative activity against human MDA-MB-435/LCC6MDR cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
    [PMID: 34371464]
    MDA-MB-435 IC50
    2.4 μM
    Compound: YM-155
    Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
    Antiproliferative activity against human MDA-MB-435 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
    [PMID: 34371464]
    PC-3 EC50
    92 nM
    Compound: YM155
    Cytotoxicity against human PC3 cells by MTT assay
    Cytotoxicity against human PC3 cells by MTT assay
    [PMID: 28774426]
    Vero C1008 CC50
    400 μM
    Compound: 27; YM155
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay
    [PMID: 35620927]
    體外研究
    (In Vitro)

    Sepantronium bromide (YM155;30 μM) 對(duì)存活基因啟動(dòng)子驅(qū)動(dòng)的熒光素酶報(bào)告基因活性不敏感。Sepantronium bromide 通過存活蛋白基因啟動(dòng)子的轉(zhuǎn)錄抑制,顯著抑制 p53 缺陷的 PC-3 和 PPC-1 人 HRPC 細(xì)胞中的內(nèi)源性存活蛋白表達(dá)。Sepantronium bromide (100 nM) 不影響 c-IAP2、XIAP、Bcl-2、Bcl-xL、Bad、α-肌動(dòng)蛋白和 β-微管蛋白的蛋白表達(dá)。Sepantronium bromide 有效抑制人類癌細(xì)胞系 (突變或截短的 p53),例如 PC-3、PPC-1、DU145、TSU-Pr1、22Rv1、SK-MEL-5 和 A375,IC50范圍分別為 2.3 到 11 nM[1]。
    Sepantronium bromide (YM155) 導(dǎo)致 NSCLC 細(xì)胞對(duì) γ 輻射的敏感性增加。Sepantronium bromide 結(jié)合 γ 輻射可增加凋亡細(xì)胞的數(shù)量和 caspase-3 的活性。此外,Sepantronium bromide 可延遲核 DNA 中輻射誘導(dǎo)的雙鏈斷裂的修復(fù)[2]。

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

    體內(nèi)研究
    (In Vivo)

    Sepantronium bromide (YM155;3 和 10 mg/kg) 抑制 PC-3 異種移植物中的腫瘤生長(zhǎng),沒有明顯的體重減輕和血細(xì)胞計(jì)數(shù)減少。Sepantronium bromide 在體內(nèi)高度分布于腫瘤組織。Sepantronium bromide 在 PC-3 原位異種移植物中以 5 mg/kg 的劑量顯示出 80% 的 TGI[1]。
    Sepantronium bromide (YM155) 與 γ 輻射結(jié)合顯示出有效的抗腫瘤活性針對(duì)裸鼠中的 H460 或 Calu6 異種移植物[2]
    在這種原位腎和轉(zhuǎn)移性肺腫瘤模型中,Sepantronium bromide (YM-155) 和 IL-2 相加地降低了腫瘤重量、肺轉(zhuǎn)移和熒光素染色的腫瘤圖像[3]。

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

    Clinical Trial
    分子量

    443.29

    Formula

    C20H19BrN4O3

    CAS 號(hào)
    性狀

    固體

    顏色

    Light yellow to green yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (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 (112.79 mM; 超聲助溶)

    DMSO 中的溶解度 : 11.67 mg/mL (26.33 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2559 mL 11.2793 mL 22.5586 mL
    5 mM 0.4512 mL 2.2559 mL 4.5117 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 (sealed storage, away from moisture)。-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):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
    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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (4.51 mM); 澄清溶液

      此方案可獲得 ≥ 2 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

      Solubility: 2 mg/mL (4.51 mM); 澄清溶液; 超聲助溶

      此方案可獲得 2 mg/mL的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 20.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

    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: 50 mg/mL (112.79 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

    純度: 99.36%

    參考文獻(xiàn)
    Cell Assay
    [1]

    The antiproliferative activity of Sepantronium bromide is measured. After treatment with Sepantronium bromide for 48 h, the cell count is determined by sulforhodamine B assay. The GI50 value is calculated by logistic analysis, which is the drug concentration resulting in a 50% reduction in the net protein increase (as measured by sulforhodamine B staining) in control cells during the drug incubation. The assay is done in triplicate, and the mean GI50 value is obtained from the results of four independent assays.

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

    Animal Administration
    [1]

    Five-week-old male nude mice (BALB/c nu/nu) are used for the assay. PC-3 cells (2×106-3×106) are injected into the flanks of the mice and allowed to reach a tumor volume of > 100 mm3 in tumor volume (length×width2×0.5). Sepantronium bromide is s.c. administered as a 3-day continuous infusion per week for 2 weeks using an implanted micro-osmotic pump or i.v. administered five times a week for 2 weeks. The percentage of tumor growth inhibition 14 days after initial Sepantronium bromide administration is calculated for each group using the following formula: MTV=100×{1-[(MTV of the treated group on day 14)-(MTV of the treated group on day 0)]/[(MTV of the control group on day 14)-(MTV of the control group on day 0)]}, where MTV is mean tumor volume. For both the frozen tumors and plasma samples, survivin expression levels are analyzed by Western blotting and Sepantronium bromide concentration by high-performance liquid chromatography/triple quadrupole mass spectrometry (LC/MS/MS) using validated methods.

    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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-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
    DMSO / H2O 1 mM 2.2559 mL 11.2793 mL 22.5586 mL 56.3965 mL
    5 mM 0.4512 mL 2.2559 mL 4.5117 mL 11.2793 mL
    10 mM 0.2256 mL 1.1279 mL 2.2559 mL 5.6396 mL
    15 mM 0.1504 mL 0.7520 mL 1.5039 mL 3.7598 mL
    20 mM 0.1128 mL 0.5640 mL 1.1279 mL 2.8198 mL
    25 mM 0.0902 mL 0.4512 mL 0.9023 mL 2.2559 mL
    H2O 30 mM 0.0752 mL 0.3760 mL 0.7520 mL 1.8799 mL
    40 mM 0.0564 mL 0.2820 mL 0.5640 mL 1.4099 mL
    50 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1279 mL
    60 mM 0.0376 mL 0.1880 mL 0.3760 mL 0.9399 mL
    80 mM 0.0282 mL 0.1410 mL 0.2820 mL 0.7050 mL
    100 mM 0.0226 mL 0.1128 mL 0.2256 mL 0.5640 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。

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    產(chǎn)品名稱:
    Sepantronium bromide
    目錄號(hào):
    HY-10194
    需求量: