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  1. Neuronal Signaling Stem Cell/Wnt
  2. Notch
  3. FLI-06

FLI-06是Notch信號(hào)傳導(dǎo)的抑制劑,EC50值為2.3 μM。

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FLI-06 Chemical Structure

FLI-06 Chemical Structure

CAS No. : 313967-18-9

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥880
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5 mg ¥800
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10 mg ¥1200
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50 mg ¥4000
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Customer Review

    FLI-06 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Nov;107:1370-1376.  [Abstract]

    ECa109 and EC9706 cells are treated with different concentrations of FLI-06 (0, 10 and 20 μM) for 48 h, respectively. The expressions of Notch3, DTX1 and Hes1 are investigated by Western blotting.

    FLI-06 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Nov;107:1370-1376.  [Abstract]

    ECa109 and EC9706 cells are treated with different concentrations of FLI-06 (0, 10 and 20 μM) for 48 h, respectively. The expressions of LSD1 and H3K4me2 are investigated by Western blotting.
    • 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

    FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.

    IC50 & Target

    EC50: 2.3 μM (Notch signaling)[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    1.8 μM
    Compound: 1; FLI-06
    Antiproliferative activity against human HCT116 cells after 72 hrs by SYBR green dye based fluorescence assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by SYBR green dye based fluorescence assay
    [PMID: 30201292]
    HeLa IC50
    2.3 μM
    Compound: 6; FLI-06
    Inhibition of gamma secretase mediated Notch delta E activation in human HeLa cells expressing EGFP after 16 hrs by immunofluorescence analysis
    Inhibition of gamma secretase mediated Notch delta E activation in human HeLa cells expressing EGFP after 16 hrs by immunofluorescence analysis
    [PMID: 27045975]
    體外研究
    (In Vitro)

    FLI-06, disrupted the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. FLI-06 inhibited general secretion at a step before exit from the endoplasmic reticulum. In FLI-06–treated cells, no APPCTF accumulates despite strongly reduced Aβ secretion, suggesting that it acts upstream of α-secretase and β-secretase cleavage. FLI-06 is a very useful chemical probe to study the inhibition of membrane traffic at pre- ER-exit site (ERES) stages without fusion of ER-Golgi[1].

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

    分子量

    438.52

    Formula

    C25H30N2O5

    CAS 號(hào)
    性狀

    固體

    顏色

    Light yellow to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : ≥ 38 mg/mL (86.66 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    * "≥" 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 2.2804 mL 11.4020 mL 22.8040 mL
    5 mM 0.4561 mL 2.2804 mL 4.5608 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, 2 years; -20°C, 1 year。-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)?年內(nèi)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(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: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (5.70 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 25.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.70 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    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(guò)程有損耗,建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    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,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料
    參考文獻(xiàn)
    Kinase Assay
    [1]

    EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1].

    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, 2 years; -20°C, 1 year。-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)?年內(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 1 mM 2.2804 mL 11.4020 mL 22.8040 mL 57.0099 mL
    5 mM 0.4561 mL 2.2804 mL 4.5608 mL 11.4020 mL
    10 mM 0.2280 mL 1.1402 mL 2.2804 mL 5.7010 mL
    15 mM 0.1520 mL 0.7601 mL 1.5203 mL 3.8007 mL
    20 mM 0.1140 mL 0.5701 mL 1.1402 mL 2.8505 mL
    25 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2804 mL
    30 mM 0.0760 mL 0.3801 mL 0.7601 mL 1.9003 mL
    40 mM 0.0570 mL 0.2850 mL 0.5701 mL 1.4252 mL
    50 mM 0.0456 mL 0.2280 mL 0.4561 mL 1.1402 mL
    60 mM 0.0380 mL 0.1900 mL 0.3801 mL 0.9502 mL
    80 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7126 mL
    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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    Inquiry Information

    產(chǎn)品名稱:
    FLI-06
    目錄號(hào):
    HY-15860
    需求量: