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

Saracatinib (Synonyms: AZD0530)

Cat. No.: HY-10234 Purity: 99.47%
Data Sheet SDS 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

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10 mM * 1 mL in DMSO $66 In-stock
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50 mg $150 In-stock
100 mg $240 In-stock
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Description

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
NCT Number Sponsor Condition Start Date Phase
NCT00704366 AstraZeneca Solid Tumor June 2008 Phase 1
NCT02167256 Yale University|Alzheimer's Therapeutic Research Institute Alzheimer's Disease December 2014 Phase 2
NCT00771979 AstraZeneca Healthy November 2008 Phase 1
NCT02262026 Yale University Alcoholism November 2014 Phase 1
NCT00558272 AstraZeneca Breast Cancer|Prostate Cancer|Bone Neoplasms February 2008 Phase 2
NCT00475956 AstraZeneca Neoplasms May 2007 Phase 1
NCT01000896 AstraZeneca Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer January 2010 Phase 1
NCT01216176 Joyce Marie Slingerland|Stanford University|University of Miami Breast Cancer October 2008 Phase 1|Phase 2
NCT00853983 AstraZeneca Healthy March 2009 Phase 1
NCT00610714 AstraZeneca Ovarian Neoplasms|Ovarian Cancer April 2008 Phase 2
NCT00265876 NCIC Clinical Trials Group|Canadian Cancer Trials Group Pancreatic Cancer September 2005 Phase 1|Phase 2
NCT00496028 AstraZeneca Neoplasms March 2007 Phase 1
NCT00704366 AstraZeneca Solid Tumor June 2008 Phase 1
NCT02167256 Yale University|Alzheimer's Therapeutic Research Institute Alzheimer's Disease December 2014 Phase 2
NCT00771979 AstraZeneca Healthy November 2008 Phase 1
NCT02262026 Yale University Alcoholism November 2014 Phase 1
NCT00558272 AstraZeneca Breast Cancer|Prostate Cancer|Bone Neoplasms February 2008 Phase 2
NCT00475956 AstraZeneca Neoplasms May 2007 Phase 1
NCT01000896 AstraZeneca Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer January 2010 Phase 1
NCT01216176 Joyce Marie Slingerland|Stanford University|University of Miami Breast Cancer October 2008 Phase 1|Phase 2
NCT00853983 AstraZeneca Healthy March 2009 Phase 1
NCT00610714 AstraZeneca Ovarian Neoplasms|Ovarian Cancer April 2008 Phase 2
NCT00265876 NCIC Clinical Trials Group|Canadian Cancer Trials Group Pancreatic Cancer September 2005 Phase 1|Phase 2
NCT00496028 AstraZeneca Neoplasms March 2007 Phase 1
NCT02116712 Tony Eissa|University of Texas|University of Cincinnati|Baylor College of Medicine Pulmonary Lymphangioleiomyomatosis August 2014 Phase 1
NCT02737202 Baylor College of Medicine|University of Cincinnati|Brigham and Women's Hospital|Stanford University|Loyola University|University of South Florida|National Institutes of Health (NIH) Pulmonary Lymphangioleiomyomatosis April 2016 Phase 2
NCT00669019 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIA Melanoma|Stage IIB Melanoma|Stage IIC Melanoma|Stage IV Melanoma July 2006 Phase 2
NCT02732587 Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Alcohol Drinking November 2015 Phase 1
NCT00607594 National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|Adenocarcinoma of the Stomach|Recurrent Gastric Cancer|Stage III Gastric Cancer|Stage III Esophageal Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer January 2008 Phase 2
NCT01864655 Stephen M. Strittmatter|Yale University Alzheimer's Disease July 2013 Phase 1
NCT00638937 National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer February 2008 Phase 2
NCT00718809 National Cancer Institute (NCI) Invasive Thymoma and Thymic Carcinoma|Recurrent Thymoma and Thymic Carcinoma|Stage III Thymoma|Stage IVA Thymoma|Stage IVB Thymoma June 2008 Phase 2
NCT00528645 National Cancer Institute (NCI) Extensive Stage Small Cell Lung Cancer|Lung Metastases|Malignant Pleural Effusion|Recurrent Small Cell Lung Cancer November 2007 Phase 2
NCT02955186 Yale University Alcohol Drinking May 9, 2017 Phase 2
NCT01267266 National Cancer Institute (NCI) Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer December 2010 Phase 2
NCT02085603 Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca Cancer March 2014 Phase 2
NCT00513435 National Cancer Institute (NCI) Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity|Recurrent Verrucous C July 2007 Phase 2
NCT00559507 National Cancer Institute (NCI) Estrogen Receptor-negative Breast Cancer|Male Breast Cancer|Progesterone Receptor-negative Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer October 2007 Phase 2
NCT00397878 National Cancer Institute (NCI) Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer November 2006 Phase 2
NCT00513071 National Cancer Institute (NCI) Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer August 2007 Phase 2
NCT00659360 National Cancer Institute (NCI) Adult Fibrosarcoma|Adult Leiomyosarcoma|Adult Liposarcoma|Adult Malignant Fibrous Histiocytoma|Adult Rhabdomyosarcoma|Dermatofibrosarcoma Protuberans|Endometrial Stromal Sarcoma|Recurrent Adult Soft Tissue Sarcoma|Recurrent Uterine Sarcoma|Stage III Adult Soft Tissue Sarcoma|Stage III Uterine Sarcoma|Stage IV Adult Soft Tissue Sarcoma|Stage IV Uterine Sarcoma|Uterine Carcinosarcoma|Uterine Leiomyosarcoma February 2008 Phase 2
NCT00752206 Sarcoma Alliance for Research through Collaboration|AstraZeneca Osteosarcoma March 2009 Phase 2
NCT01196741 University College, London|AstraZeneca|Cancer Research UK Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer March 2011 Phase 2|Phase 3
NCT00735917 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer October 2008 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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]

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
[1]

Saracatinib (AZD0530) is dissolved in DMSO and diluted with saline[1].

Mice and Rat[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
M.Wt

542.03

Formula

C₂₇H₃₂ClN₅O₅

CAS No.

379231-04-6

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

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

Purity: 99.47%

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Saracatinib
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