1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. Saruparib

Saruparib  (Synonyms: AZD5305)

製品番号: HY-132167 純度: 99.76%
COA 取扱説明書 Technical Support

Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair.

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CAS 番号 : 2589531-76-8

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 330 在庫あり
Solution
10 mM * 1 mL in DMSO USD 330 在庫あり
Solid
1 mg $142 在庫あり
5 mg $300 在庫あり
10 mg $480 在庫あり
25 mg $950 在庫あり
50 mg $1450 在庫あり
100 mg $2250 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 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Saruparib purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Mar;57(3):522-529.  [Abstract]

    Dose response survival curves illustrating the cell inhibitory effects of AZD5305 (0-10 μM, 7 d) in isogenic BRCA1 mutant (mutant/HR defective) and BRCA1 revertant (HR proficient) SUM149 cells.

    Saruparib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Jun 10;122(23):e2426743122.  [Abstract]

    7-d olaparib dose–response viability assay in Brca2Δ/Δ Trp53Δ/Δ PtenΔ/Δ organoids stably expressing the indicated sgRNAs (sgNT2, Cdt1 g2-14, and Cdt1 g4-2) in LentiCRISPR-GFP treated with AZD5305.

    Saruparib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 August 25.

    Saruparib (0.1, 1, or 10 µM) treatment significantly reduced PARP-positive cells (green) in the outer nuclear layer (ONL).

    Saruparib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 August 25.

    Calpain activity-positive cells (orange) were increased by Saruparib (0.1, 1, or 10 µM) treatment.

    Saruparib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 August 25.

    ONL cell death, visualized via TUNEL assay (red), was dose-dependently increased by Saruparib (0.1, 1, or 10 µM) treatment.
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    製品説明

    Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair[1][2].

    IC50 & Target[1]

    PARP1

    3 nM (IC50)

    PARP2

    1400 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    DLD-1 IC50
    0.002 μM
    Compound: 25
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    [PMID: 34570508]
    DLD-1 IC50
    0.915 nM
    Compound: AZD5305
    Antiproliferative activity against human DLD-1 cells harbouring BRCA-2 mutant assessed as inhibition of cell growth
    Antiproliferative activity against human DLD-1 cells harbouring BRCA-2 mutant assessed as inhibition of cell growth
    [PMID: 36343904]
    DLD-1 IC50
    12.06 μM
    Compound: AZD5305
    Antiproliferative activity against human DLD-1 cells harbouring wild type BRCA assessed as inhibition of cell growth
    Antiproliferative activity against human DLD-1 cells harbouring wild type BRCA assessed as inhibition of cell growth
    [PMID: 36343904]
    体外実験

    Saruparib (AZD5305) (0.1 nM-100 μM) inhibits PARylation in A549 WT cells by selectively blocking PARP1 enzymatic activity with an IC50 value of 2.3 nM[1].
    AZD5305 (0.1 nM-100 μM; A549 WT cells) is a potent and selective trapper of PARP1 in a dose-dependent manner by single digit nanomolar concentrations[1].
    AZD5305 (0.1 nM-100 μM; 48 h; DLD1 WT and DLD1 BRCA2-/-) has anti-proliferative activity and targets cancer cells with HRR-deficiency, inducing DNA damage accumulation and cell-cycle arrest[1].

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

    体内実験

    Saruparib (AZD5305) (0.01-0.3 mg/kg; p.o.; daily, for 35 d; female Han Wistar rats) demonstrates sustained antitumor activity in BRCAm xenograft and PDX models in vivo[1].

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

    Animal Model: Female Han Wistar rats with BRCAm xenograft and PDX models (12-13 weeks of age)[1]
    Dosage: 0.01, 0.03, 0.1, and 0.3 mg/kg
    Administration: Oral administration; daily, for 35 days
    Result: Had antitumor efficacy in a dose-dependent manner.
    臨床実験
    分子量

    406.48

    分子式

    C22H26N6O2

    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=NC=C(N2CCN(CC3=CC(N4)=C(N=C3)C=C(CC)C4=O)CC2)C=C1)NC

    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 : 25 mg/mL (61.50 mM; ultrasonic and warming and heat to 60°C; 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 2.4601 mL 12.3007 mL 24.6015 mL
    5 mM 0.4920 mL 2.4601 mL 4.9203 mL
    10 mM 0.2460 mL 1.2301 mL 2.4601 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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    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)

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    体積 (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: ≥ 1 mg/mL (2.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.46 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
    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: 99.76%

    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. 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 2.4601 mL 12.3007 mL 24.6015 mL 61.5036 mL
    5 mM 0.4920 mL 2.4601 mL 4.9203 mL 12.3007 mL
    10 mM 0.2460 mL 1.2301 mL 2.4601 mL 6.1504 mL
    15 mM 0.1640 mL 0.8200 mL 1.6401 mL 4.1002 mL
    20 mM 0.1230 mL 0.6150 mL 1.2301 mL 3.0752 mL
    25 mM 0.0984 mL 0.4920 mL 0.9841 mL 2.4601 mL
    30 mM 0.0820 mL 0.4100 mL 0.8200 mL 2.0501 mL
    40 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5376 mL
    50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2301 mL
    60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0251 mL
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    • Molarity Calculator

    • Dilution Calculator

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

    質量   濃度   体積   分子量 *
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    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.

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    製品名:
    Saruparib
    製品番号:
    HY-132167
    数量:
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