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  2. Immunology/Inflammation Apoptosis Anti-infection
  3. CD47 Apoptosis Parasite
  4. RRx-001

RRx-001 是一種低氧選擇性的表觀遺傳因子，被用作放射或化療敏感劑，能誘發(fā)凋亡，克服骨髓瘤的耐藥性。RRx-001 具有有效的抗癌活性且毒性極低。RRx-001是一個(gè)免疫檢查點(diǎn)的抑制劑，可下調(diào) CD47 和SIRP-α。RRx-001是G6PD的有效抑制劑，具有較強(qiáng)的抗瘧活性。

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RRx-001 Chemical Structure

RRx-001 Chemical Structure

CAS No. : 925206-65-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥500
In-stock
5 mg ￥1100
In-stock
10 mg ￥1650
In-stock
50 mg ￥4894
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

    RRx-001 purchased from MCE. Usage Cited in: J Virol. 2023 Feb 16;e0001623.  [Abstract]

    RRx-001 (2.5, 5, 10, 20, 100 μM; 12 h) significantly and dose-dependently reduces Newcastle disease virus (NDV) NP protein expression in NDV-infected cells.

    RRx-001 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.  [Abstract]

    Whole cell lysates from J82 shCCDC6 or shCTRL cells, treated with different concentrations of RRx-001, or untreated, are immunoblotted with anti-CCDC6 antibody. γH2AX levels are shown. Tubulin is used as loading control.

    RRx-001 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90.  [Abstract]

    Protein levels of DNMT1 and CCDC6 in J82 cells treated with different concentrations of RRx-001, as determined by western blot. Vinculin and Tubulin are used as internal controls for sample loading. 5-AZA is used as positive control for inhibition of DNMT1 expression.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity[3].

    IC50 & Target

    Plasmodium

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A498 IC50
    4.9 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    A549 IC50
    6.00 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    HT-29 IC50
    3.4 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    IMR-32 IC50
    5.1 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    M21 IC50
    2.6 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    MCF7 IC50
    4.00 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    PANC-1 IC50
    2.3 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    RKO IC50
    3.00 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    SCC-7 IC50
    1.8 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    SNB-75 IC50
    3.8 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    U-87MG ATCC IC50
    2.7 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    UMSCC22B IC50
    2.3 pM
    Compound: RRx-001; ABDNAZ
    Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay
    Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay
    		[PMID: 34043360]
    體外研究
    (In Vitro)

    RRx-001 (0-5 μM，24 小時(shí)) 抑制 MM 細(xì)胞生長(zhǎng)并克服對(duì)新型和常規(guī)療法的耐藥性[1]。
    RRx-001 阻斷 MM 細(xì)胞的遷移和相關(guān)的血管生成[1]。
    RRx-001 誘導(dǎo)顯著的 G1 期生長(zhǎng)停滯，并伴隨 S 期減少。RRx-001 引發(fā) MM 細(xì)胞顯著凋亡[1]。
    RRx-001 通過(guò)下調(diào)DNA甲基轉(zhuǎn)移酶抑制DNA甲基化[1]。
    RRx-001 和 RRx-001 處理的巨噬細(xì)胞上清液下調(diào)腫瘤細(xì)胞上的 CD47 和巨噬細(xì)胞上的 SIRPα[2]。

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

    Cell Viability Assay[1]

    Cell Line: Human MM-cell lines (MM.1S, RPMI-8226, H929, ARP1, KMS-11, OPM2, LR5, ANBL6.WT), along with drug resistant cell lines such as (MM.1R, Dox40, LR5, ANBL6.BR, RPMI-8226).
    Concentration: 0-5 μM.
    Incubation Time: 24 hours.
    Result: Induced a dose-dependent significant (p < 0.05) decrease in viability of all cell lines.
    體內(nèi)研究
    (In Vivo)

    RRx-001 (5 mg/kg 或 10 mg/kg，靜脈注射，每周三次，持續(xù) 24 天) 在異種移植小鼠模型中抑制腫瘤生長(zhǎng)并延長(zhǎng)存活期[1]。
    RRx-001 (10 mg/kg，IP，每周兩次和每天一次) 對(duì) A549 肺癌模型表現(xiàn)出有效的抗癌活性，這取決于腫瘤組織中是否存在腫瘤相關(guān)巨噬細(xì)胞 (TAM)[2]。

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

    Animal Model: CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 106 MM.1S cells in 100 μL of serum-free RPMI 1640 medium[1].
    Dosage: 5 mg/kg or 10 mg/kg.
    Administration: I.V., thrice-weekly for 24 days.
    Result: Blocked MM tumor growth and enhances survival.
    Treatment was well tolerated, suggested by no apparent weight loss.
    Animal Model: Female BALB/c nude mice (19.2?±?1.7?g) based on A549 lung cancer model[2].
    Dosage: 10?mg/kg.
    Administration: IP, twice a week and once a day.
    Result: Resulted in the most significant tumor growth retardation.
    Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.
    Clinical Trial
    分子量

    268.02

    Formula

    C5H6BrN3O5
    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (373.11 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(kāi)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 3.7311 mL 18.6553 mL 37.3107 mL
    5 mM 0.7462 mL 3.7311 mL 7.4621 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。-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。

    • 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 (9.33 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(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 (9.33 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(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

    只
    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)

    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。-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
    DMSO 1 mM 3.7311 mL 18.6553 mL 37.3106 mL 93.2766 mL
    5 mM 0.7462 mL 3.7311 mL 7.4621 mL 18.6553 mL
    10 mM 0.3731 mL 1.8655 mL 3.7311 mL 9.3277 mL
    15 mM 0.2487 mL 1.2437 mL 2.4874 mL 6.2184 mL
    20 mM 0.1866 mL 0.9328 mL 1.8655 mL 4.6638 mL
    25 mM 0.1492 mL 0.7462 mL 1.4924 mL 3.7311 mL
    30 mM 0.1244 mL 0.6218 mL 1.2437 mL 3.1092 mL
    40 mM 0.0933 mL 0.4664 mL 0.9328 mL 2.3319 mL
    50 mM 0.0746 mL 0.3731 mL 0.7462 mL 1.8655 mL
    60 mM 0.0622 mL 0.3109 mL 0.6218 mL 1.5546 mL
    80 mM 0.0466 mL 0.2332 mL 0.4664 mL 1.1660 mL
    100 mM 0.0373 mL 0.1866 mL 0.3731 mL 0.9328 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：
    RRx-001
    目錄號(hào)：
    HY-16438
    需求量：