| Field | Specification |
|---|---|
| Alternative names | AZD0530 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H32ClN5O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Saracatinib, also known as AZD0530, is a potent Src family inhibitor with IC50 values ranging from 2.7 nM to 11 nM against c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. It shows high selectivity over other tyrosine kinases[1]. It is supplied as a white to light yellow solid (C27H32ClN5O5, MW 542.03) at 99.23% purity.
Physical & Chemical Properties
| CAS Number | 379231-04-6 |
|---|---|
| Molecular Formula | C27H32ClN5O5 |
| Molecular Weight | 542.03 g/mol |
| Purity | 99.23% |
| Appearance | Solid |
| Color | White to light yellow |
| SMILES | ClC1=CC=C2C(OCO2)=C1NC3=C4C(OC5CCOCC5)=CC(OCCN6CCN(C)CC6)=CC4=NC=N3 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Autophagy |
| Solubility | In Vitro: DMSO: 50 mg/mL (92.25 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 2.7 nM (Src), 30 nM (v-Abl), 66 nM (EGFR), 200 nM (c-Kit)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (92.25 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.61 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (4.61 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.61 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Saracatinib (AZD0530), an orally available Src inhibitor, shows potent antimigratory and anti-invasive effects in vitro and inhibits metastasis in a murine bladder cancer model. Its antiproliferative activity differs among cell lines (IC50 of 0.2-10 μM). Proliferation of Src3T3 mouse fibroblasts is potently inhibited by Saracatinib, while its antiproliferative activity varies across a panel of human cancer cell lines containing endogenous Src. Five of the human cancer cell lines tested (tumor types: colon, prostate, lung, and leukemia) show sub micromolar growth inhibition with Saracatinib, with IC50 values of 0.2-0.7 μM. K562, a Bcr-Abl-driven human leukemia cell line, is inhibited by Saracatinib with an IC50 of 0.22 μM in 3-day MTS cell proliferation assays. Migration of human lung cancer A549 cells is lowered by Saracatinib in the microdroplet migration assay, in a concentration-dependent manner (IC50 0.14 μM)[1].
In Vivo
Saracatinib (AZD0530) potently inhibits proliferation of subcutaneously transplanted Src3T3 fibroblasts in mice and rats, in a dose-dependent manner. Significant tumor growth inhibition is seen in both models at doses ≥6 mg/kg/day (inhibition of 60% in mice and 98% in rats relative to vehicle-treated animals), and complete inhibition of tumor growth occurs at the maximum doses investigated: 100% at 25 mg/kg/day in mice and at 10 mg/kg/day in rats[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
To examine the reversibility and mechanism of Saracatinib inhibition, use a full-length activated human Src in a continuous, coupled assay. Vary ATP and peptide substrate (Src II peptide) concentrations in turn (ATP 40-1280 μM; Src II peptide 100-800 μM) together with Saracatinib (0-30 nM), keeping the non-varied substrate at saturating concentration (ATP 1.6 mM; Src II peptide 1.0 mM). Use a BIAcore inhibition-in-solution assay to measure Saracatinib binding to inactivated Src (phosphorylated at tyrosine 527, not tyrosine 416); the assay follows competition between Saracatinib and an immobilized ureidoquinazoline for Src binding. Analyze data by unweighted nonlinear regression using GraFit, version 5, and use an F-test to identify the most suitable equation[1].
Cell Assay[1]
Assess cell proliferation with a colorimetric 5-bromo-2′-deoxyuridine (BrdU) Cell Proliferation ELISA kit. Plate cells onto 96-well plates (1.5×104 cells/well); the following day, add 0.039-20 μM Saracatinib in DMSO (final concentration 0.5%) and incubate the cells for 24 h. Pulse label the cells with BrdU for 2 h and fix. Denature cellular DNA with the provided solution and incubate with antiBrdU peroxidase for 90 min. After three washes with phosphate-buffered saline, add tetramethylbenzidine substrate solution and incubate the plates on a plate shaker for 10-30 min, until absorbance of the positive control reaches approximately 1.5 absorbance units at 690 nm[1].
Animal Administration[1]
Mice and Rats[1] Use female athymic mice (nu/nu) and rats (RH-rnu/rnu). Treat animals once daily by oral gavage with vehicle alone or Saracatinib 6.25-50 mg/kg for 10-91 days. Calculate tumor growth inhibition. For pharmacokinetic and pharmacodynamic analysis, humanely sacrifice the animals and collect samples (plasma and tumor). Homogenize tumor samples with 5 volumes of water and extract with chloroform. After solid-phase extraction, analyze plasma and tumor samples for Saracatinib concentration by high-performance liquid chromatography with tandem mass spectrometric detection.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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B-lymphoid tyrosine kinase-mediated FAM83A phosphorylation elevates pancreatic tumorigenesis through interacting with β-catenin. Signal Transduct Target Ther 2023 Feb 17;8(1):66. PMID: 36797256
Osimertinib covalently binds to CD34 and eliminates myeloid leukemia stem/progenitor cells. Cancer Res 2024 Feb 1;84(3):479-492. PMID: 38095536
p38 mediated ACSL4 phosphorylation drives stress-induced esophageal squamous cell carcinoma growth through Src myristoylation. Nat Commun 2025 Apr 7;16(1):3319. PMID: 40195298
TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. Nat Commun 2023 Apr 24;14(1):2342. PMID: 37095176
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med 2018 Jul 18;10(450):eaaq1093.
MBD3 deficiency decommissions the NuRD complex and orchestrates the epigenetic regulation of gene expression to suppress neuroblastoma progression. Neuro Oncol 2026 Jan 7:noaf297. PMID: 41499431
Enhanced ferroptosis sensitivity promotes the formation of highly myopic cataract via the DDR2-Hippo pathway. Cell Death Dis 2025 Feb 3;16(1):64. PMID: 39900894
Hippo signaling suppresses tumor cell metastasis via a Yki-Src42A positive feedback loop. Cell Death Dis 2021 Dec 3;12(12):1126. PMID: 34862372
FYN is required for ARHGEF16 to promote proliferation and migration in colon cancer cells. Cell Death Dis 2020 Aug 7;11(8):652. PMID: 32811808
Macrophage KDM2A promotes atherosclerosis via regulating FYN and inducing inflammatory response. Int J Biol Sci 2025 Mar 31;21(6):2780-2805. PMID: 40303308
