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

Saracatinib (Synonyms: AZD0530)

Cat. No.: HY-10234 Purity: 99.88%
Handling Instructions

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 and 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 72 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 288 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Top Publications Citing Use of Products

    Saracatinib purchased from MCE. Usage Cited in: Arch Biochem Biophys. 2018 May 1;645:54-60.

    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.

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

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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 and shows high selectivity over other tyrosine kinases.

    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 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].

    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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (59.04 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1845 mL 0.9225 mL 1.8449 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Saracatinib is prepared in 1.25% polyethylene glycol, 2.5% Tween-80, and 5% DMSO[2].

    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
    Molecular Weight

    542.03

    Formula

    C₂₇H₃₂ClN₅O₅

    CAS No.

    379231-04-6

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.88%

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    Product Name:
    Saracatinib
    Cat. No.:
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    Cat. No.: HY-10234