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  1. Apoptosis Autophagy
  2. Bcl-2 Family Apoptosis Autophagy Mitophagy
  3. ABT-737

ABT-737 是一種 BH3 模擬物,是一種有效的 Bcl-2、Bcl-xLBcl-w 抑制劑,EC50 分別為 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 誘導(dǎo) BCL-2/BAX 復(fù)合物的破壞和 BAK 依賴性但不依賴 BIM 的內(nèi)在凋亡途徑激活。ABT-737 誘導(dǎo)自噬,并且具有用于急性髓系白血病 (AML) 研究的潛力。

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ABT-737 Chemical Structure

ABT-737 Chemical Structure

CAS No. : 852808-04-9

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Customer Review

Other Forms of ABT-737:

MCE 顧客使用本產(chǎn)品發(fā)表的 47 篇科研文獻(xiàn)

WB

    ABT-737 purchased from MCE. Usage Cited in: Cancer Lett. 2019 Oct 1;461:102-111.  [Abstract]

    Expression of active (cleaved) PARP and active (cleaved) Caspase-3 after 48h of treatment with AGS, 1 μM ABT-737 or 1 μM ABT-737 added to AGS as determined by Western blot. Floating cells are included in lysate.

    查看 Bcl-2 Family 亞型特異性產(chǎn)品:

    • 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

    ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research[1][2][3].

    IC50 & Target[1]

    Bcl-2

    30.3 nM (EC50)

    Bcl-xL

    78.7 nM (EC50)

    Bcl-W

    197.8 nM (EC50)

    Bcl-B

    1820 nM (EC50)

    Bfl-1

    >10 μM (EC50)

    Mcl-1

    >10 μM (EC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CCRF-CEM IC50
    0.74 μM
    Compound: 1, ABT-737
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    DU-145 IC50
    27.6 μM
    Compound: 7, ABT-737
    Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    FL5.12 EC50
    30 nM
    Compound: 1, ABT-737
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum
    [PMID: 18841882]
    FL5.12 EC50
    7.7 nM
    Compound: 1, ABT-737
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum
    Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum
    [PMID: 18841882]
    HCT-116 IC50
    4.06 μM
    Compound: 7, ABT-737
    Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    HCT-116 IC50
    47.7 μM
    Compound: ABT-737
    Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    HL-60 IC50
    0.76 μM
    Compound: 1, ABT-737
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    HL-60 IC50
    0.97 μM
    Compound: ABT-737
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    Jurkat IC50
    1.38 μM
    Compound: 7, ABT-737
    Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    K562 IC50
    16.4 μM
    Compound: ABT-737
    Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry
    Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry
    [PMID: 23314054]
    K562 IC50
    34.7 μM
    Compound: 1, ABT-737
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay
    [PMID: 22582991]
    Leukemia cell IC50
    > 1 μM
    Compound: 1, ABT-737
    Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay
    Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay
    [PMID: 23767404]
    Leukemia cell IC50
    > 10 μM
    Compound: 1, ABT-737
    Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay
    Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay
    [PMID: 23767404]
    MCF7 IC50
    21.26 μM
    Compound: 7, ABT-737
    Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    MCF7 IC50
    25.33 μM
    Compound: ABT-737
    Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
    Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    MCF7 EC50
    4.39 μM
    Compound: ABT-737
    Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 35421577]
    MDA-MB-435 IC50
    > 122.94 μM
    Compound: ABT-737
    Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    MEF EC50
    > 10000 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum
    [PMID: 21366295]
    MEF EC50
    > 10000 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum
    Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum
    [PMID: 21366295]
    MEF EC50
    0.013 μM
    Compound: 1; ABT-737
    Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis
    Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis
    [PMID: 33904752]
    MEF EC50
    2.03 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum
    [PMID: 21366295]
    MEF EC50
    51 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum
    [PMID: 21366295]
    MEF EC50
    51 nM
    Compound: 1, ABT-737
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum
    Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum
    [PMID: 21366295]
    MOLT-4 IC50
    227 nM
    Compound: ABT-263
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    NCI-H1417 IC50
    0.13 μM
    Compound: 1, ABT-737
    Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay
    Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay
    [PMID: 22448988]
    NCI-H1417 IC50
    173.4 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1417 IC50
    412 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H146 EC50
    0.087 μM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum
    Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum
    [PMID: 18841882]
    NCI-H146 IC50
    0.097 μM
    Compound: 1, ABT-737
    Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay
    Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay
    [PMID: 22448988]
    NCI-H146 IC50
    37 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H146 IC50
    43.8 nM
    Compound: ABT-263
    Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    NCI-H187 IC50
    137.7 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1963 IC50
    54 nM
    Compound: 1, ABT-737
    Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
    Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
    [PMID: 23448298]
    NCI-H1963 IC50
    59 nM
    Compound: 1, ABT-737
    Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay
    Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay
    [PMID: 22747598]
    NCI-H23 IC50
    71.16 μM
    Compound: ABT-737
    Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay
    Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    NCI-H460 IC50
    8.03 μM
    Compound: 7, ABT-737
    Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    Platelet IC50
    242 nM
    Compound: ABT-263
    Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    Raji IC50
    93.49 μM
    Compound: ABT-737
    Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay
    [PMID: 22172701]
    RS4-11 IC50
    0.27 μM
    Compound: ABT-737
    Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry
    Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry
    [PMID: 23314054]
    RS4-11 IC50
    0.33 μM
    Compound: ABT-737
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    [PMID: 29453135]
    RS4-11 IC50
    49 nM
    Compound: ABT-263
    Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay
    [PMID: 32145645]
    SK-OV-3 IC50
    46.59 μM
    Compound: ABT-737
    Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay
    Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    SU.86.86 IC50
    4.24 μM
    Compound: 7, ABT-737
    Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay
    Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay
    [PMID: 19743858]
    U-266 IC50
    27.35 μM
    Compound: ABT-737
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    [PMID: 27712939]
    體外研究
    (In Vitro)

    ABT-737 與 BCL-2、BCL-XLBCL-W 具有高親和力 (Ki<1 nM),但與其他抗凋亡 BCL-2 家族成員(包括 MCL-1 和 BFL-1)的結(jié)合力較弱 (Ki>460 nM)。ABT-737 與 BCL-XLBCL-2 的 BH3 結(jié)合槽結(jié)合[1]。
    ABT-737(100 nM;1-72 小時)誘導(dǎo) HL-60 細(xì)胞凋亡并與化療產(chǎn)生協(xié)同作用[1]。
    ABT-737(5、7.5、10 μM;72 小時)導(dǎo)致約 80% 的 HCT116 細(xì)胞死亡。BAX 敲除變體對 ABT-737 具有完全抗性[1]
    ABT-737 對細(xì)胞周期分布沒有影響。ABT-737 破壞 BCL-2/BAX 異二聚化并誘導(dǎo) HL-60 白血病細(xì)胞中的 BAX 構(gòu)象變化[1]。
    ABT-737 可誘導(dǎo)敏感細(xì)胞中 BAX/BAK 依賴性最大 O2 消耗率受損。MCF10A 細(xì)胞中穩(wěn)定的 BCL-2 過表達(dá)可誘導(dǎo) ABT-737 敏感的死亡狀態(tài)。ABT-737 可誘導(dǎo) B 細(xì)胞淋巴瘤細(xì)胞中劑量依賴性最大 O2 消耗率受損[3]。

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

    體內(nèi)研究
    (In Vivo)

    ABT-737(20、30 mg/kg/天;腹腔注射;持續(xù) 21 天)在 20 和 30 mg/kg 劑量水平下分別可抑制 4 至 6 周齡 CB.17 Scid 小鼠(患有人類白血病 KG-1 細(xì)胞)的白血病負(fù)擔(dān) 48% 和 53%[1]。
    ABT-737 顯著延長了這種惡性白血病模型中小鼠的生存期[1]。

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

    分子量

    813.43

    Formula

    C42H45ClN6O5S2

    CAS 號
    性狀

    固體

    顏色

    Yellow to orange

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    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 : 66.67 mg/mL (81.96 mM; 超聲助溶 (<60°C); 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 1.2294 mL 6.1468 mL 12.2936 mL
    5 mM 0.2459 mL 1.2294 mL 2.4587 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, 2 years; -20°C, 1 year。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?jiān)?年內(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(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)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(shí)驗(yàn)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(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

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

      Solubility: 2.5 mg/mL (3.07 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (3.07 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。
    動物溶解方案計算器
    請輸入動物實(shí)驗(yàn)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

    由于實(shí)驗(yàn)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 +
    +
    %
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    %
    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)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)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(shí)驗(yàn)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(jǐn)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: 99.96%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    To determine the binding affinity of GST-BCL-2 family proteins to the FITC-conjugated BH3 domain of BIM (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR), FPAs are performed as follows. Briefly, 100 nM of GST-BCL-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. IC50s are determined using GraphPad Prism software.

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

    Cell Assay
    [3]

    Cells are treated with ABT-737, ABT-263, or vehicle (DMSO) for 4 h in XF24 assay medium (6×104?MCF10A cells, see medium composition below) or RPMI 1640 medium (1×106?B-cell lymphoma cells) and apoptosis is analyzed by Annexin-V-binding/PI exclusion or by sub-diploid nuclei determination. FACS analysis is performed on Becton Dickinson FACScan or FACScalibur instruments. Data analysis is performed with CellQuest software.

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

    Animal Administration
    [1]

    For intraperitoneal (i.p.) administration, 1 g/mL?stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4?5; final concentration of DMSO ≤ 1%). Mice injected with FD/ΔRaf-1:ER cells are treated with either ABT-737 (20 and 30 mg/kg/mouse every day i.p. for 21 days starting on day 1 post-cell injection (n=9-10 mice per group) or vehicle or left untreated (control); mice injected with human KG-1 cells are treated with 30 mg/kg ABT-737 starting on day 18 post-cell injection. For noninvasive imaging of FD/ΔRaf-1:ER-luc?cells, anesthetized mice are injected with 150 mg/kg of D-luciferin and placed for imaging in the In Vivo Imaging System with total imaging time of 2 min.

    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;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, 2 years; -20°C, 1 year。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?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 1.2294 mL 6.1468 mL 12.2936 mL 30.7341 mL
    5 mM 0.2459 mL 1.2294 mL 2.4587 mL 6.1468 mL
    10 mM 0.1229 mL 0.6147 mL 1.2294 mL 3.0734 mL
    15 mM 0.0820 mL 0.4098 mL 0.8196 mL 2.0489 mL
    20 mM 0.0615 mL 0.3073 mL 0.6147 mL 1.5367 mL
    25 mM 0.0492 mL 0.2459 mL 0.4917 mL 1.2294 mL
    30 mM 0.0410 mL 0.2049 mL 0.4098 mL 1.0245 mL
    40 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7684 mL
    50 mM 0.0246 mL 0.1229 mL 0.2459 mL 0.6147 mL
    60 mM 0.0205 mL 0.1024 mL 0.2049 mL 0.5122 mL
    80 mM 0.0154 mL 0.0768 mL 0.1537 mL 0.3842 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:
    ABT-737
    目錄號:
    HY-50907
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