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  2. Neuronal Signaling Stem Cell/Wnt
  3. γ-secretase Notch
  4. RO4929097

RO4929097 (RG-4733) 是一種 γ secretase 抑制劑，IC50 值為 4 nM，能夠抑制細胞內(nèi) Aβ40 的產(chǎn)生和 Notch 活性，EC50 值分別為 14 nM 和 5 nM。

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RO4929097 Chemical Structure

RO4929097 Chemical Structure

CAS No. : 847925-91-1

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥826
In-stock
1 mg ￥419
In-stock
5 mg ￥800
In-stock
10 mg ￥1440
In-stock
25 mg ￥2600
In-stock
50 mg ￥3900
In-stock
100 mg ￥5850
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

    RO4929097 purchased from MCE. Usage Cited in: FASEB J. 2017 Sep;31(9):3774-3786.  [Abstract]

    Western blot analysis of E-cadherin, vimentin, Slug, and Twist1 in BGC823 cells treated with RO4929097 in addition to miR-2392 inhibition.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively[1].

    IC50 & Target

    IC50: 4 nM (γ secretase)[1]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 EC50
    14 nM
    Compound: 12; RO4929097
    Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA
    Inhibition of gamma secretase in HEK293 cells expressing APP695 assessed as reduction in amyloid beta (1 to 40 residues) by ELISA
    		[PMID: 27045975]
    HEK293 EC50
    5 nM
    Compound: 12; RO4929097
    Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay
    Inhibition of gamma secretase mediated Notch1 signaling in HEK293 cells expressing truncated human Notch1 by luciferase reporter gene assay
    		[PMID: 27045975]
    體外研究
    (In Vitro)

    RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells[1].?RO4929097 (1 μM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells[2]. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors[1]. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 104 cells in vivo[3].

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

    469.40

    Formula

    C22H20F5N3O3
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : ≥ 49 mg/mL (104.39 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.1304 mL 10.6519 mL 21.3038 mL
    5 mM 0.4261 mL 2.1304 mL 4.2608 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    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

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.33 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。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.33 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，此方案實驗周期在半個月以上的動物實驗酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲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

    純度: 98.64%

    參考文獻
    Cell Assay
    [2]

    The IBC cell lines SUM149 and SUM190 are seeded at a density of 5 × 104?cells. The next day, they are treated with vehicle or increasing doses of RO4929097, ranging from 0.1 nM to 10 μM. After 72 hrs, cells are trypsinized and viable cells counted with a hemocytometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: RO4929097-treated mice are orally dosed with suspensions at 3 to 60 mg/kg RO4929097 according to the indicated regimens. In the Calu-6 xenograft model, RO4929097 is dosed at 60 mg/kg/d every other week for 4 weeks (7+/7- × 2 cycles). For all other xenograft models, RO4929097 is dosed once daily at 10 mg/kg for 21 days. Statistical analysis is determined by Mann-Whitney rank-sum test, one-way ANOVA, and post hoc Bonferroni?t?test. Differences between groups are considered significant when?P?≤ 0.05. A549 tumors from vehicle-treated and selected RO4929097-treated groups are collected and fixed in 10% zinc-formalin overnight, processed, paraffin-embedded, sectioned at 5 μM, and stained with H&E for histopathology assessment. An Olympus BX51 microscope (×40 objective) mounted with a Nikon DS-Fi1 using the NIS-Elements F2.20 program collected the histology pictures. For Western blot analysis, three A549 tumors from each group, 7 (60 mg/kg) or 21 days (3 and 30 mg/kg), are flash-frozen. Collagen type V is detected using the H-200 antibody at a dilution of 1:1,000, and MFAP5 is detected using the antibody at a dilution of 1:1,000.

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

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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 1 mM 2.1304 mL 10.6519 mL 21.3038 mL 53.2595 mL
    5 mM 0.4261 mL 2.1304 mL 4.2608 mL 10.6519 mL
    10 mM 0.2130 mL 1.0652 mL 2.1304 mL 5.3259 mL
    15 mM 0.1420 mL 0.7101 mL 1.4203 mL 3.5506 mL
    20 mM 0.1065 mL 0.5326 mL 1.0652 mL 2.6630 mL
    25 mM 0.0852 mL 0.4261 mL 0.8522 mL 2.1304 mL
    30 mM 0.0710 mL 0.3551 mL 0.7101 mL 1.7753 mL
    40 mM 0.0533 mL 0.2663 mL 0.5326 mL 1.3315 mL
    50 mM 0.0426 mL 0.2130 mL 0.4261 mL 1.0652 mL
    60 mM 0.0355 mL 0.1775 mL 0.3551 mL 0.8877 mL
    80 mM 0.0266 mL 0.1331 mL 0.2663 mL 0.6657 mL
    100 mM 0.0213 mL 0.1065 mL 0.2130 mL 0.5326 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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    產(chǎn)品名稱：
    RO4929097
    目錄號：
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