2. Apoptosis
  3. IAP Apoptosis
  4. AZD5582

AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

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CAS 番号 : 1258392-53-8

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5 mg $90 在庫あり
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カスタマーレビュー

Based on 16 publication(s) in Google Scholar

Other Forms of AZD5582:

AZD5582 関連抗体

Top Publications Citing Use of Products

    AZD5582 purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2023 Apr 3;11(4):450-465.  [Abstract]

    AZD5582 (0.1-1 μM; 24 h) decreases the expression of cIAP1, cIAP2 and XIAP in GM-CSF DCs.

    AZD5582 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2022 Apr;100(4):629-643.  [Abstract]

    Evaluation of cell growth inhibition by AZD5582 on a panel of 6 cell lines including 5 cancer lines (Huh7, M231, H727, HepG2, and A549) and 1 normal line (MSC). Cells were treated by AZD5582 at indicated series of concentration for 24 h and then analyzed for cell viability and proliferation by CCK-8 kit.

    AZD5582 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2022 Apr;100(4):629-643.  [Abstract]

    AZD5582 (20 nM). Detection of FITC-phalloidin (green) labeled filamentous actin (F-actin) cytoskeleton in Huh7 cells.

    AZD5582 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2022 Apr;100(4):629-643.  [Abstract]

    AZD5582 (20 nM). The expression levels of activated caspase-8 (C-Casp-8), -9 (C-Casp-9), and -3 (C-Casp-3) in Huh7 cells were compared using flow cytometry with a specific FITC-labeled inhibitor.

    AZD5582 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2022 Apr;100(4):629-643.  [Abstract]

    Cells were treated with vector (Ctrl), 2.0 ng/mL EV-T TRAIL (EV-T) and/or 20 nM AZD5582 (AZD)/(Combi) for 24 hours, respectively, followed by Western blotting analysis using antibodies against cFLIP, BC1-2, MCl-1, Survivin, cIAP-1, XIAP, and GAPDH. Huh7 cells were treated and analyzed.

    AZD5582 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2022 Apr;100(4):629-643.  [Abstract]

    Tumor growth/volume curves. Each treatment comprises of intratumoral injection per animal of 100 μL saline vehicle (Ctrl), 8.0 ng EV-T TRAIL (EV-T), 2.0 μg AZD5582 (AZD), or the combination of AZD and EV-T (Combi), respectively, and total three injections were performed with a 48-h interval.

    IAP アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    cIAP cIAP-1 cIAP-2 XIAP

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis[1].

    IC50 & Target[1]

    cIAP1

    15 nM (IC50)

    cIAP2

    21 nM (IC50)

    XIAP

    15 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    MDA-MB-231 EC50
    0.1 nM
    Compound: 14, AZD5582
    Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA
    Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA
    		[PMID: 24320998]
    MDA-MB-231 GI50
    < 0.06 nM
    Compound: 14, AZD5582
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay
    		[PMID: 24320998]
    体外実験

    AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[2].
    AZD5582 (20 nM; 17 or 25 hours) downregulates cIAP-1, activates RIPK1 (upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7[2].
    AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells[2].

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

    AZD5582 関連抗体

    Cell Viability Assay[2]

    Cell Line: H1975 NSCLC cell line
    Concentration: 20 nM
    Incubation Time: 48 hours
    Result: Cooperated with IFNγ or viral double-stranded RNA (dsRNA) to inhibit cell viability even cell death.

    Apoptosis Analysis[2]

    Cell Line: HCC827 NSCLC cell line
    Concentration: 20 nM
    Incubation Time: 48 hours
    Result: Had an inhibitory effect on cell viability by cooperating with IFNγ.

    Western Blot Analysis[2]

    Cell Line: H1975 NSCLC cell line
    Concentration: 20 nM
    Incubation Time: 17 or 25 hours
    Result: Down-regulated cIAP-1, activated RIPK1 (upstream regulator of caspase-8), triggered the cleavage (activation) of caspase-3,7,8 and 9.
    体内実験

    AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved; when the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect[1].

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

    Animal Model: MDA-MB-231 xenograft-bearing mice[1]
    Dosage: 0.1 mg/kg, 0.5 mg/kg, 3.0 mg/kg
    Administration: Intravenous injection; once a week; 2 weeks
    Result: Resulted in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg
    分子量

    1015.29

    分子式

    C58H78N8O8
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CN[C@@H](C)C(N[C@H](C(N1[C@H](C(N[C@H]2C3=CC=CC=C3C[C@H]2OCC#CC#CCO[C@H]4[C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@H](C)NC)=O)C6CCCCC6)=O)=O)C(C=CC=C7)=C7C4)=O)CCC1)=O)C8CCCCC8)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (98.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.9849 mL 4.9247 mL 9.8494 mL
    5 mM 0.1970 mL 0.9849 mL 1.9699 mL
    10 mM 0.0985 mL 0.4925 mL 0.9849 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 50 mg/mL (49.25 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 0.9849 mL 4.9247 mL 9.8494 mL 24.6235 mL
    5 mM 0.1970 mL 0.9849 mL 1.9699 mL 4.9247 mL
    10 mM 0.0985 mL 0.4925 mL 0.9849 mL 2.4624 mL
    15 mM 0.0657 mL 0.3283 mL 0.6566 mL 1.6416 mL
    20 mM 0.0492 mL 0.2462 mL 0.4925 mL 1.2312 mL
    25 mM 0.0394 mL 0.1970 mL 0.3940 mL 0.9849 mL
    30 mM 0.0328 mL 0.1642 mL 0.3283 mL 0.8208 mL
    40 mM 0.0246 mL 0.1231 mL 0.2462 mL 0.6156 mL
    50 mM 0.0197 mL 0.0985 mL 0.1970 mL 0.4925 mL
    60 mM 0.0164 mL 0.0821 mL 0.1642 mL 0.4104 mL
    80 mM 0.0123 mL 0.0616 mL 0.1231 mL 0.3078 mL
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    AZD5582 Related Classifications

    • Molarity Calculator

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    一般には略語で表示されます：C1V1 = C2V2

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    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.

    Keywords:

    AZD55821258392-53-8AZD 5582AZD-5582IAPApoptosisInhibitorinhibitorinhibit

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    製品名:
    AZD5582
    製品番号:
    HY-12600
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