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> Saruparib [2589531-76-8]

Saruparib [2589531-76-8]

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Cat# HY-132167-1mL

Size : 10mM/1mL

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

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]
In Vitro

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.

Saruparib Related Antibodies

Solvent & Solubility
In Vitro: 

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
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.

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.
Purity & Documentation
References

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