2. Cell Cycle/DNA Damage
  3. CDK
  4. AZD4573

AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.

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CAS 番号 : 2057509-72-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 418 在庫あり
Solution
10 mM * 1 mL in DMSO USD 418 在庫あり
Solid
1 mg $180 在庫あり
5 mg $380 在庫あり
10 mg $590 在庫あり
50 mg $950 在庫あり
100 mg $1500 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

AZD4573 関連抗体

Top Publications Citing Use of Products

    AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189.  [Abstract]

    qPCR data showing the expression levels of TC target genes after AZD4573 (300 nM) treatment.

    AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189.  [Abstract]

    AZD4573 (300 nM) displayed a significant reduction in TC nuclear immunofluorescence.

    AZD4573 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2024 Sep 13;30(18):4179-4189.  [Abstract]

    AZD4573 (300 nM) reduced TC levels by Immunoblotting.

    AZD4573 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Jan 2;84(1):17-25.  [Abstract]

    At the indicated concentrations. Cell viability was assessed using CellTiter-Glo (day 7). Data represent percentage NVP-2/AZD4573–treated viable cells compared with vehicle control.

    AZD4573 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Apr 7;31(1):107485.  [Abstract]

    Survival analysis of atuveciclib and AZD4573 (20 mg/kg, i.p.)-treated cohorts versus vehicle control.

    CDK 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
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    • 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

    AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies[1].

    IC50 & Target[1]

    CDK9

    4 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    4T1 IC50
    8.29 1
    Compound: AZD4573
    Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
    Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay
    		[PMID: 38885173]
    OPM-2 GI50
    23 1
    Compound: 16; AZD-4573
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    		[PMID: 32866383]
    OPM-2 GI50
    23 1
    Compound: 16; AZD-4573
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    		[PMID: 32866383]
    BT-549 IC50
    9.57 1
    Compound: AZD4573
    Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
    Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay
    		[PMID: 38885173]
    T-cell IC50
    < 4 1
    Compound: 54; AZD-4573
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    		[PMID: 35485642]
    T-cell IC50
    <4 1
    Compound: 54; AZD-4573
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    		[PMID: 35485642]
    MDA-MB-468 IC50
    13.57 1
    Compound: AZD4573
    Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
    Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay
    		[PMID: 38885173]
    MM1.S IC50
    6.03 1
    Compound: AZD4573
    Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
    Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay
    		[PMID: 38885173]
    OPM-2 GI50
    23 1
    Compound: 16; AZD-4573
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    Growth inhibition of human OPM-2 cells incubated for 24 hrs
    		[PMID: 32866383]
    T-cell IC50
    < 4 1
    Compound: 54; AZD-4573
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    Inhibition of CDK9/Cyclin T (unknown origin) in presence of ATP by Kinomescan assay
    		[PMID: 35485642]
    体外実験

    Short-term treatment with AZD4573 led to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 13.7 nM in an acute myeloid leukemia model MV4-11) [1].

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

    AZD4573 関連抗体
    体内実験

    AZD4573 exhibits a short half-life in multiple species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    429.94

    分子式

    C22H28ClN5O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CN=C(NC([C@H]2CCC[C@@H](NC(C)=O)C2)=O)C=C1C3=C(CC(C)(C)C4)N4N=C3
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (116.30 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 2.3259 mL 11.6295 mL 23.2591 mL
    5 mM 0.4652 mL 2.3259 mL 4.6518 mL
    10 mM 0.2326 mL 1.1630 mL 2.3259 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    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: ≥ 2.08 mg/mL (4.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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).
    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

    純度: 99.98%

    COA (252 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3259 mL 11.6295 mL 23.2591 mL 58.1476 mL
    5 mM 0.4652 mL 2.3259 mL 4.6518 mL 11.6295 mL
    10 mM 0.2326 mL 1.1630 mL 2.3259 mL 5.8148 mL
    15 mM 0.1551 mL 0.7753 mL 1.5506 mL 3.8765 mL
    20 mM 0.1163 mL 0.5815 mL 1.1630 mL 2.9074 mL
    25 mM 0.0930 mL 0.4652 mL 0.9304 mL 2.3259 mL
    30 mM 0.0775 mL 0.3877 mL 0.7753 mL 1.9383 mL
    40 mM 0.0581 mL 0.2907 mL 0.5815 mL 1.4537 mL
    50 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1630 mL
    60 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9691 mL
    80 mM 0.0291 mL 0.1454 mL 0.2907 mL 0.7268 mL
    100 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5815 mL
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    • Your name will appear on the site.

    AZD4573 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    AZD45732057509-72-3AZD 4573AZD-4573CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    製品名:
    AZD4573
    製品番号:
    HY-112088
    数量:
    MCE 日本正規代理店:

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