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  2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Proteasome Autophagy Apoptosis
  4. Carfilzomib

Carfilzomib  (Synonyms: 卡非佐米; PR-171)

目錄號: HY-10455 純度: 99.98%
COA 產(chǎn)品使用指南 技術(shù)支持

Carfilzomib (PR-171) 是不可逆的蛋白酶體 (proteasome) 抑制劑，其在ANBL-6和RPMI 8226細(xì)胞中的 IC50 為5 nM。

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Carfilzomib Chemical Structure

Carfilzomib Chemical Structure

CAS No. : 868540-17-4

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
5 mg ￥640
In-stock
10 mg ￥1020
In-stock
25 mg ￥1888
In-stock
50 mg ￥2850
In-stock
100 mg ￥4500
In-stock
200 mg 現(xiàn)貨 詢價
500 mg   詢價  
1 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Carfilzomib:

MCE 顧客使用本產(chǎn)品發(fā)表的 38 篇科研文獻(xiàn)

WB

    Carfilzomib purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.  [Abstract]

    J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 μM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.

    Carfilzomib purchased from MCE. Usage Cited in: J Agric Food Chem. 2017 Jun 7;65(22):4384-4394.  [Abstract]

    Resveratrol activates the HSF1 signaling pathway. J-Lat A2 cells are treated with various concentrations of Resveratrol or Carfilzomib (50 nM) for 48 h. Then the cells are lysed and Ser320 phosphorylated HSF1 and total HSF1 are detected by Western blot with corresponding antibodies.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

    IC50 & Target

    IC50: 5 nM (Proteasome)
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-431 IC50
    23.8 nM
    Compound: Carfilzomib
    Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
    Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
    		[PMID: 26231162]
    A549 IC50
    43.3 nM
    Compound: Carfilzomib
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    CCRF-CEM IC50
    6.1 nM
    Compound: Carfilzomib
    Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
    Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
    		[PMID: 26231162]
    HCT-116 IC50
    19.3 nM
    Compound: Carfilzomib
    Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
    		[PMID: 26231162]
    HCT-116 IC50
    9.6 nM
    Compound: Carfilzomib
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    LP-1 IC50
    22.7 nM
    Compound: Carfilzomib
    Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay
    Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    MCF7 IC50
    0.0041 μM
    Compound: Cfz
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 30165344]
    MDA-MB-231 IC50
    0.0044 μM
    Compound: Cfz
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    		[PMID: 30165344]
    MES-SA IC50
    18 nM
    Compound: 2
    Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 19348473]
    MES-SA IC50
    413 nM
    Compound: 2
    Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 19348473]
    MGC-803 IC50
    934 nM
    Compound: Carfilzomib
    Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay
    Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    MM1.S IC50
    < 1 nM
    Compound: 2
    Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
    Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
    		[PMID: 30611983]
    MM1.S IC50
    1.5 nM
    Compound: Carfilzomib
    Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay
    Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay
    		[PMID: 28027531]
    MM1.S IC50
    1.5 nM
    Compound: Carfilzomib
    Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay
    Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay
    		[PMID: 27765408]
    MM1.S IC50
    14.35 nM
    Compound: Carfilzomib
    Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    		[PMID: 33223460]
    MM1.S IC50
    2.3 nM
    Compound: Carfilzomib
    Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
    Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    MOLT-4 IC50
    5.1 nM
    Compound: 2
    Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay
    Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay
    		[PMID: 19348473]
    NCI-H23 IC50
    0.018 μM
    Compound: Cfz
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    NCI-H727 IC50
    0.6102 μM
    Compound: Cfz
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    NCI-H929 IC50
    116.1 nM
    Compound: Carfilzomib
    Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    NCI-H929 IC50
    13.9 nM
    Compound: Carfilzomib
    Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    		[PMID: 33223460]
    NCI-H929 IC50
    21.32 nM
    Compound: Carfilzomib
    Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
    Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
    		[PMID: 24767818]
    PC-3 IC50
    23.9 nM
    Compound: Carfilzomib
    Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    RKO IC50
    27.1 nM
    Compound: Carfilzomib
    Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
    Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
    		[PMID: 26231162]
    RPMI-8226 IC50
    0.0067 μM
    Compound: Cfz
    Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay
    Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay
    		[PMID: 30165344]
    RPMI-8226 IC50
    0.007 μM
    Compound: Cfz
    Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    RPMI-8226 IC50
    13.19 nM
    Compound: Carfilzomib
    Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
    Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
    		[PMID: 24767818]
    RPMI-8226 IC50
    13.2 nM
    Compound: Carfilzomib
    Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay
    Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay
    		[PMID: 28027531]
    RPMI-8226 IC50
    13.2 nM
    Compound: Carfilzomib
    Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay
    Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay
    		[PMID: 27765408]
    RPMI-8226 IC50
    14.1 nM
    Compound: Carfilzomib
    Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
    		[PMID: 33223460]
    RPMI-8226 IC50
    2 nM
    Compound: 2
    Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
    Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
    		[PMID: 30611983]
    RPMI-8226 IC50
    2.1 nM
    Compound: Carfilzomib
    Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
    Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
    		[PMID: 30639896]
    RPMI-8226 IC50
    39.1 nM
    Compound: Kyprolis(R)
    Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
    Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
    		[PMID: 31383629]
    TOV21G IC50
    23.8 nM
    Compound: Carfilzomib
    Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
    Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
    		[PMID: 26231162]
    U-266 IC50
    35.7 nM
    Compound: Kyprolis(R)
    Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
    Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay
    		[PMID: 31383629]
    體外研究
    (In Vitro)

    Carfilzomib 在體外顯示出對 β5 亞基中 ChT-L 活性的優(yōu)先抑制效力，在 10 nM 和更高劑量時抑制超過 80%，在劑量高達(dá) 100 nM 時對 PGPH 和 TL 活性影響很小或沒有影響。Carfilzomib 降低 ANBL-6、RPMI 8226 細(xì)胞、U266 和 KAS-6/1 細(xì)胞的活力，IC50 小于 5 nM。Carfilzomib 克服了 Dex 耐藥性，因為 MM1.R 細(xì)胞的 IC50 為 15.2 nM，低于親本 MM1.S 細(xì)胞的 29.3 nM 值[1]。
    與 carfilzomib 和 HDACI 共同處理導(dǎo)致在各種套細(xì)胞淋巴瘤細(xì)胞系和原代套細(xì)胞淋巴瘤細(xì)胞中協(xié)同誘導(dǎo)細(xì)胞死亡。在 HF-4B 和 Granta 細(xì)胞中，Carfilzomib 或 ONX0912 與伏立諾他聯(lián)合處理可顯著增加半胱天冬酶活化、PARP 裂解、JNK 活化、MnSOD2 誘導(dǎo)和 DNA 損傷[2]。

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

    Carfilzomib (2.0 mg/kg，iv) 與 70 mg/kg Vorinostat 聯(lián)用幾乎消除了 Granta-luciferace 細(xì)胞異種移植模型中的腫瘤生長。與使用單一藥物或毒性極小的對照組相比，聯(lián)合處理可顯著減少生物發(fā)光[2]。

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

    719.91

    Formula

    C40H57N5O7
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    卡非佐米
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years

    *該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : 125 mg/mL (173.63 mM; 超聲助溶; 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)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.3891 mL 6.9453 mL 13.8906 mL
    5 mM 0.2778 mL 1.3891 mL 2.7781 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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    • 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(dāng)?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(dāng)保存；體內(nèi)實驗的工作液，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

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

      Solubility: 2.5 mg/mL (3.47 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。

      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 (3.47 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。

    掃碼獲得
    動物溶解方案

    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， PEG300/PEG400，Tween 80，均可在 MCE 網(wǎng)站選購。
    純度 & 產(chǎn)品資料

    純度: 99.98%

    參考文獻(xiàn)
    Cell Assay
    [1]

    WST-1 is used to determine the effects of proteasome inhibitors on cell proliferation according to the manufacturer's protocol. The inhibition of proliferation is calculated in relation to parallel control cells that receive vehicle alone and tabulated in KaleidaGraph 3.0.1 or Excel 2000. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR=IC50(resistant cells)/IC50(sensitive cells).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Animal studies are performed utilizing Beige-nude-XID mice. 10×106?Granta514 cells are pelleted, washed twice with 1X PBS, injected subcutaneously into the right flank. Once the tumors are visible, 5 to 6 mice are treated with carfilzomib±vorinostat and progress of tumor growth or regression is monitored. Stock vorinostat and carfilzomib is dissolved in DMSO and 10% sulfobutylether betacyclodextrin in 10 mM citrate buffer pH respectively. They are stored in ?80°C in small aliquots and diluted before injection.

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

    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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.3891 mL 6.9453 mL 13.8906 mL 34.7266 mL
    5 mM 0.2778 mL 1.3891 mL 2.7781 mL 6.9453 mL
    10 mM 0.1389 mL 0.6945 mL 1.3891 mL 3.4727 mL
    15 mM 0.0926 mL 0.4630 mL 0.9260 mL 2.3151 mL
    20 mM 0.0695 mL 0.3473 mL 0.6945 mL 1.7363 mL
    25 mM 0.0556 mL 0.2778 mL 0.5556 mL 1.3891 mL
    30 mM 0.0463 mL 0.2315 mL 0.4630 mL 1.1576 mL
    40 mM 0.0347 mL 0.1736 mL 0.3473 mL 0.8682 mL
    50 mM 0.0278 mL 0.1389 mL 0.2778 mL 0.6945 mL
    60 mM 0.0232 mL 0.1158 mL 0.2315 mL 0.5788 mL
    80 mM 0.0174 mL 0.0868 mL 0.1736 mL 0.4341 mL
    100 mM 0.0139 mL 0.0695 mL 0.1389 mL 0.3473 mL

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    產(chǎn)品名稱：
    Carfilzomib
    目錄號：
    HY-10455
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