1. Protein Tyrosine Kinase/RTK Autophagy
  2. Src Autophagy
  3. Saracatinib

Saracatinib  (Synonyms: AZD0530)

Cat. No.: HY-10234 Purity: 99.92%
COA Handling Instructions

Saracatinib (AZD0530) est un inhibiteur puissant de la famille Src avec des IC50s de 2,7 à 11 nM pour c-Src, Lck, c-YES, Lyn, Fyn, Fgr, et Blk. Saracatinib présente une sélectivité élevée par rapport aux autres tyrosine kinases.

Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases.

For research use only. We do not sell to patients.

Saracatinib Chemical Structure

Saracatinib Chemical Structure

CAS No. : 379231-04-6

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Solid
5 mg USD 46 In-stock
10 mg USD 72 In-stock
50 mg USD 180 In-stock
100 mg USD 288 In-stock
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500 mg   Get quote  

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Saracatinib:

Top Publications Citing Use of Products

    Saracatinib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2023 Feb 17;8(1):66.  [Abstract]

    Saracatinib (10 μM) reduces BLK-mediated FAM83A tyrosine phosphorylation in HEK293T cells.

    Saracatinib purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Apr;23(4):2399-2409.  [Abstract]

    Immunoblot analysis of p-JNK1/2 (T183/Y185) in HepG2 cells treated with saracatinib (10 μM, 12 h) and PP1 (10 μM, 2 h).

    Saracatinib purchased from MedChemExpress. Usage Cited in: Arch Biochem Biophys. 2018 May 1;645:54-60.  [Abstract]

    SK-BR-3, MCF-7, and MDA-MB-231 cells are treated with 1 μM Saracatinib for 48 h. After treatment, the Src protein expression is determined by western blot.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases[1].

    IC50 & Target

    IC50: 2.7 nM (Src), 30 nM (v-Abl), 66 nM (EGFR), 200 nM (c-Kit)[1]

    In Vitro

    Saracatinib (AZD0530), an orally available Src inhibitor, demonstrates potent antimigratory and anti-invasive effects in vitro, and inhibits metastasis in a murine model of bladder cancer. Antiproliferative activity of Saracatinib varies between cell lines (IC50 of 0.2-10 μM). Saracatinib potently inhibits the proliferation of Src3T3 mouse fibroblasts and demonstrates variable antiproliferative activity in a range of human cancer cell lines containing endogenous Src. Sub micromolar growth inhibition of five of the human cancer cell lines tested with Saracatinib (tumor types: colon, prostate, lung, and leukemia) is observed with IC50 values of 0.2-0.7 μM. In 3-day MTS cell proliferation assays, Saracatinib inhibits proliferation of the Bcr-Abl-driven human leukemia cell line K562 with an IC50 of 0.22 μM. In the microdroplet migration assay, Saracatinib reduces the migration of human lung cancer A549 cells in a concentration-dependent manner (IC50 0.14 μM)[1].

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

    In Vivo

    Saracatinib (AZD0530) treatment potently inhibits the proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats in a dose-dependent manner. In both models, significant inhibition of tumor growth is seen at doses ≥6 mg/kg/day (60% inhibition in mice and 98% inhibition in rats versus animals treated with vehicle) and, at the maximum doses investigated, complete tumor growth inhibition is observed (100% inhibition at 25 mg/kg/day in mice and 10 mg/kg/day in rats)[1].

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

    Clinical Trial
    Molecular Weight

    542.03

    Formula

    C27H32ClN5O5

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    ClC1=CC=C2C(OCO2)=C1NC3=C4C(OC5CCOCC5)=CC(OCCN6CCN(C)CC6)=CC4=NC=N3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (92.25 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 1.8449 mL 9.2246 mL 18.4492 mL
    5 mM 0.3690 mL 1.8449 mL 3.6898 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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 (4.61 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 (4.61 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    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 +
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    %
    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.
    Purity & Documentation

    Purity: 99.92%

    References
    Kinase Assay
    [1]

    Investigation of the reversibility and the mechanism of Saracatinib inhibition is conducted using a full-length activated human Src in a continuous, coupled assay. ATP and peptide substrate (Src II peptide) concentrations are varied in turn (ATP 40-1280 μM; Src II peptide 100-800 μM), in conjunction with Saracatinib (0-30 nM), at saturating concentrations of the non-varied substrate (ATP 1.6 mM; Src II peptide 1.0 mM). The binding affinity of Saracatinib for inactivated Src (phosphorylated at tyrosine 527, not tyrosine 416) is measured using a BIAcore inhibition-in-solution assay. The assay followed competition binding between Saracatinib and an immobilized ureidoquinazoline for binding to Src. Data analysis is performed by unweighted nonlinear regression using GraFit, version 5 and an F-test is used to identify the most suitable equation[1].

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

    Cell Assay
    [1]

    Cell proliferation is assessed using a colorimetric 5-bromo-2′-deoxyuridine (BrdU) Cell Proliferation ELISA kit. Briefly, cells are plated onto 96-well plates (1.5×104 cells/well), the following day 0.039-20 μM Saracatinib in DMSO (at a final concentration of 0.5%) is added and the cells are incubated for 24 h. The cells are pulse labeled with BrdU for 2 h and fixed. Cellular DNA is then denatured with the provided solution and incubated with antiBrdU peroxidase for 90 min. Following three washes with phosphate-buffered saline, tetramethylbenzidine substrate solution is added and the plates are incubated on a plate shaker for 10-30 min until the positive control absorbance at 690 nm is approximately 1.5 absorbance units[1].

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

    Animal Administration
    [1]

    Mice and Rats[1]
    Female athymic mice (nu/nu) and rats (RH-rnu/rnu) are used. Animals are treated once daily by oral gavage with either vehicle alone or Saracatinib 6.25-50 mg/kg for 10-91 days. Tumor growth inhibition is calculated. For pharmacokinetic and pharmacodynamic analysis animals are humanely sacrificed and samples (plasma and tumor) are collected. Tumor samples are homogenized with 5 volumes of water and extracted with chloroform. Plasma and tumor samples are analyzed for Saracatinib concentration using high-performance liquid chromatography with tandem mass spectrometric detection after solid-phase extraction.

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

    References

    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 1.8449 mL 9.2246 mL 18.4492 mL 46.1229 mL
    5 mM 0.3690 mL 1.8449 mL 3.6898 mL 9.2246 mL
    10 mM 0.1845 mL 0.9225 mL 1.8449 mL 4.6123 mL
    15 mM 0.1230 mL 0.6150 mL 1.2299 mL 3.0749 mL
    20 mM 0.0922 mL 0.4612 mL 0.9225 mL 2.3061 mL
    25 mM 0.0738 mL 0.3690 mL 0.7380 mL 1.8449 mL
    30 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5374 mL
    40 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1531 mL
    50 mM 0.0369 mL 0.1845 mL 0.3690 mL 0.9225 mL
    60 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL
    80 mM 0.0231 mL 0.1153 mL 0.2306 mL 0.5765 mL
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    Saracatinib Related Classifications

    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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