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  2. Metabolic Enzyme/Protease Autophagy
  3. Proteasome Autophagy
  4. Ixazomib

Ixazomib  (Synonyms: 艾沙佐米; MLN2238)

目錄號(hào): HY-10453 純度: 99.06%
COA 產(chǎn)品使用指南 技術(shù)支持

Ixazomib (MLN2238) 是一種有效的選擇性的可逆蛋白酶體 (proteasome)抑制劑，抑制20S蛋白酶體的糜蛋白酶樣蛋白水解 (β5) 位點(diǎn)，IC50 為 3.4 nM，Ki 為 0.93 nM。

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Ixazomib Chemical Structure

Ixazomib Chemical Structure

CAS No. : 1072833-77-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥477
In-stock
1 mg ￥272
In-stock
5 mg ￥600
In-stock
10 mg ￥900
In-stock
25 mg ￥1800
In-stock
50 mg ￥2700
In-stock
100 mg ￥4188
In-stock
500 mg 現(xiàn)貨 詢價(jià)
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Ixazomib:

    Ixazomib purchased from MCE. Usage Cited in: Elife. 2019 Mar 12;8:e44161.  [Abstract]

    Cell lines are treated with DMSO, bortezomib or MLN2238 for 48 hours. c-MYC protein levels in RPMI8226, a multiple myeloma cell line, decrease following proteasome inhibition by immunoblot.

    • 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

    Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).

    IC50 & Target

    IC50: 3.4 nM (20S proteasome)[1]
    Ki: 0.93 nM (20S proteasome)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    ARH-77 IC50
    65.5 nM
    Compound: MLN2238
    Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 29934218]
    Calu-6 IC50
    9 nM
    Compound: MLN2238
    Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay
    Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay
    		10.1039/C2MD20060K
    HEK293 IC50
    6.2 nM
    Compound: MLN2238
    Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control
    Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control
    		10.1039/C2MD20060K
    HeLa GI50
    181.8 μM
    Compound: MLN 2238
    Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    		[PMID: 32031798]
    HepG2 GI50
    > 200 μM
    Compound: MLN 2238
    Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    		[PMID: 32031798]
    RPMI-8226 IC50
    55.32 nM
    Compound: MLN2238
    Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 29934218]
    U-266 IC50
    52.15 nM
    Compound: MLN2238
    Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 29934218]
    體外研究
    (In Vitro)

    Ixazomib (MLN2238) 是一種 N 末端的二肽基亮氨酸硼酸，優(yōu)先結(jié)合并抑制 20S 蛋白酶體的胰凝乳蛋白酶樣蛋白水解 (β5) 位點(diǎn)，IC50 值為 3.4 nM (Ki 為 0.93 nM)。在較高濃度下，Ixazomib (MLN2238) 還抑制半胱天冬酶樣 (β1) 和胰蛋白酶樣 (β2) 蛋白水解位點(diǎn) (IC50 分別為 31 和 3，500 nM)。在多種哺乳動(dòng)物細(xì)胞系中進(jìn)行細(xì)胞活力研究，以比較 Ixazomib (MLN2238) 與 Bortezomib 的體外抗增殖作用。對(duì) A375 (肺)、H460 (肺)、HCT-116 (結(jié)腸) 和 HT-29 (結(jié)腸) 細(xì)胞進(jìn)行的研究表明，這兩種化合物的 LD50 值相似，范圍為 4-58 nM[1]。

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

    Ixazomib (MLN2238) 在 CWR22 異種移植模型中顯示出抗腫瘤活性。將以 14 mg/kg iv 或 7 mg/kg iv 給藥的 Ixazomib (MLN2238) 的抗腫瘤作用與以每周兩次方案以 0.8 mg/kg iv 或 0.4 mg/kg iv 給藥的硼替佐米進(jìn)行比較。Ixazomib (MLN2238) 和 Bortezomib (HY-10227) 的高劑量在該模型中顯示出相似的抗腫瘤活性 (T/C 分別為 0.36 和 0.44)。然而，Ixazomib (MLN2238) (7 mg/kg) 在 0.5 MTD 劑量下顯示出比 0.5 MTD 劑量的硼替佐米更有效 (0.4 mg/kg；T/C=0.49 與 T/C=0.79 相比) (MLN2238) 顯示時(shí)間依賴性可逆蛋白酶體抑制；然而，Ixazomib (MLN2238) 的蛋白酶體解離半衰期 (t1/2) 被確定為 18 分鐘[1]。

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

    361.03

    Formula

    C14H19BCl2N2O4
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    艾沙佐米
    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 : 62.5 mg/mL (173.12 mM; 超聲助溶; 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 2.7699 mL 13.8493 mL 27.6985 mL
    5 mM 0.5540 mL 2.7699 mL 5.5397 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: ≥ 2.08 mg/mL (5.76 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.76 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 20.8 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 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(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

    純度: 99.85%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 d before the start of the experiment at 10,000 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or Ixazomib in DMSO (0.5% final, v/v) for 1 h at 37°C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or Ixazomib (MLN2238) for 30 min at 37°C and then washed thrice in medium to remove the compounds. Cells are incubated for an additional 4 h at 37°C, after which the medium is removed and replaced with fresh medium. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents. Luminescence is measured using a LEADseeker instrument[1].

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

    Mice[1]
    Male CB17-SCID mice, approximately 8 to 11 wk of age, are inoculated s.c. with freshly dissected CWR22 tumor fragments (~20 mg) in the right dorsal flank. Mean tumor volume (MTV) is calculated using the following formula: 0.5×(length×width2). When MTV reaches approximately 150 to 200 mm3, animals are randomized into treatment groups (n=10 per group) before dosing. Antitumor activity is determined at the end of the study by calculating the treatment over control (T/C) ratio of their MTVs at the end of the study.
    Rats[1]
    To determine the pharmacokinetic profile of Ixazomib and Bortezomib in a second species, Sprague-Dawley rats are administered a single i.v. dose of Ixazomib (MLN2238) at either 0.3 or 0.2 mg/kg or Bortezomib at 0.2 mg/kg. Both Ixazomib doses provided a greater plasma exposure (AUC0-48h of 704 and 1,070 h?ng/mL for 0.2 and 0.3 mg/kg doses, respectively) compared with Bortezomib (AUC0-48h of 206 h?ng/mL), confirming that Ixazomib (MLN2238) also has improved plasma exposure compared with Bortezomib in rodents.

    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。-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 2.7699 mL 13.8493 mL 27.6985 mL 69.2463 mL
    5 mM 0.5540 mL 2.7699 mL 5.5397 mL 13.8493 mL
    10 mM 0.2770 mL 1.3849 mL 2.7699 mL 6.9246 mL
    15 mM 0.1847 mL 0.9233 mL 1.8466 mL 4.6164 mL
    20 mM 0.1385 mL 0.6925 mL 1.3849 mL 3.4623 mL
    25 mM 0.1108 mL 0.5540 mL 1.1079 mL 2.7699 mL
    30 mM 0.0923 mL 0.4616 mL 0.9233 mL 2.3082 mL
    40 mM 0.0692 mL 0.3462 mL 0.6925 mL 1.7312 mL
    50 mM 0.0554 mL 0.2770 mL 0.5540 mL 1.3849 mL
    60 mM 0.0462 mL 0.2308 mL 0.4616 mL 1.1541 mL
    80 mM 0.0346 mL 0.1731 mL 0.3462 mL 0.8656 mL
    100 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6925 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：
    Ixazomib
    目錄號(hào)：
    HY-10453
    需求量：