1. Protein Tyrosine Kinase/RTK
  2. Src

Saracatinib (Synonyms: AZD0530)

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

Saracatinib is a potent Src inhibitor with IC50 of 2.7 nM, also inhibits EGFRL861Q (IC50=4nM), EGFRL858R (IC50= 5nM) and v-Abl (IC50=30 nM).

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
10 mg USD 72 In-stock
50 mg USD 180 In-stock
100 mg USD 288 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

    Saracatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

    Saracatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    SCM stimulation of phospho-STAT5 and drug combination effect on phosphorylation of phospho-STAT5. Expression of phospho-STAT5 and total STAT5 in MOLM13 cells treated for 1.5 h with DMSO vehicle, PKC412 (5 nM), KIN40 (82.5 nM) or a combination of both. Results shown are representative of two independent experiments in which similar results are observed.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Saracatinib is a potent Src inhibitor with IC50 of 2.7 nM, also inhibits EGFRL861Q (IC50=4nM), EGFRL858R (IC50= 5nM) and v-Abl (IC50=30 nM).

    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
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay

    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

    Saracatinib (AZD0530) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.5%) before use[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

    Saracatinib (AZD0530) is dissolved in DMSO and diluted with saline[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.

    Molecular Weight




    CAS No.




    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 32 mg/mL

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

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


    Purity: 99.88%

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name



    Applicant name *


    Email address *

    Phone number *


    Organization name *

    Country *


    Requested quantity *


    Bulk Inquiry

    Inquiry Information

    Product Name:
    Cat. No.: