Saracatinib
Title | Journal |
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Cytochrome P450 Mediated Bioactivation of Saracatinib. | Chemical research in toxicology 20161121 |
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors. | ACS medicinal chemistry letters 20150709 |
Lipopolysaccharide-induced caveolin-1 phosphorylation-dependent increase in transcellular permeability precedes the increase in paracellular permeability. | Drug design, development and therapy 20150101 |
Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. | International journal of cancer 20130101 |
Phase I open-label study of cediranib, an oral inhibitor of VEGF signalling, in combination with the oral Src inhibitor saracatinib in patients with advanced solid tumours. | Investigational new drugs 20121001 |
Src-signaling interference impairs the dissemination of blood-borne tumor cells. | Cell and tissue research 20120801 |
Antitumor activity of Src inhibitor saracatinib (AZD-0530) in preclinical models of biliary tract carcinomas. | Molecular cancer therapeutics 20120701 |
False-negative MRI biomarkers of tumour response to targeted cancer therapeutics. | British journal of cancer 20120605 |
A phase II trial of the Src kinase inhibitor saracatinib (AZD0530) in patients with metastatic or locally advanced gastric or gastro esophageal junction (GEJ) adenocarcinoma: a trial of the PMH phase II consortium. | Investigational new drugs 20120601 |
Simultaneous targeting of Src kinase and receptor tyrosine kinase results in synergistic inhibition of renal cell carcinoma proliferation and migration. | International journal of cancer 20120601 |
Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours. | British journal of cancer 20120522 |
Role of Src in breast cancer cell migration and invasion in a breast cell/bone-derived cell microenvironment. | Breast cancer research and treatment 20120501 |
Distinct effects of saracatinib on memory CD8+ T cell differentiation. | Journal of immunology (Baltimore, Md. : 1950) 20120501 |
Common PIK3CA mutants and a novel 3' UTR mutation are associated with increased sensitivity to saracatinib. | Clinical cancer research : an official journal of the American Association for Cancer Research 20120501 |
A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer. | Investigational new drugs 20120401 |
Effects of Src kinase inhibition by saracatinib (AZD0530) on bone turnover in advanced malignancy in a Phase I study. | Bone 20120401 |
An update on dual Src/Abl inhibitors. | Future medicinal chemistry 20120401 |
TRAF6 inhibits proangiogenic signals in endothelial cells and regulates the expression of vascular endothelial growth factor. | Biochemical and biophysical research communications 20120302 |
WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors. | Laboratory investigation; a journal of technical methods and pathology 20120301 |
Modulation of epithelial tight junctions by TGF-beta 3 in cultured oral epithelial cells. | Australian dental journal 20120301 |
In silico investigation of potential SRC kinase ligands from traditional Chinese medicine. | PloS one 20120101 |
Traditional Chinese medicine as dual guardians against hypertension and cancer? | Journal of biomolecular structure & dynamics 20120101 |
Hepatitis B virus large surface antigen promotes liver carcinogenesis by activating the Src/PI3K/Akt pathway. | Cancer research 20111215 |
Phase II trial of saracatinib (AZD0530), an oral SRC-inhibitor for the treatment of patients with hormone receptor-negative metastatic breast cancer. | Clinical breast cancer 20111001 |
Expression and functional role of CRIPTO-1 in cutaneous melanoma. | British journal of cancer 20110927 |
Simultaneous exposure of transformed cells to SRC family inhibitors and CHK1 inhibitors causes cell death. | Cancer biology & therapy 20110801 |
Combined Src and ER blockade impairs human breast cancer proliferation in vitro and in vivo. | Breast cancer research and treatment 20110701 |
Current status of SRC inhibitors in solid tumor malignancies. | The oncologist 20110501 |
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors. | Bioorganic & medicinal chemistry 20110415 |
Osteoporosis: now and the future. | Lancet (London, England) 20110409 |
Phase II study of saracatinib (AZD0530) for patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC). | Anticancer research 20110101 |
Impact of the Src inhibitor saracatinib on the metastatic phenotype of a fibrosarcoma (KHT) tumor model. | Anticancer research 20101101 |
Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors. | Clinical cancer research : an official journal of the American Association for Cancer Research 20101001 |
[SRC kinases in tumor therapy]. | Medizinische Klinik (Munich, Germany : 1983) 20101001 |
Gene array and fluorescence in situ hybridization biomarkers of activity of saracatinib (AZD0530), a Src inhibitor, in a preclinical model of colorectal cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20100815 |
Novel dual Src/Abl inhibitors for hematologic and solid malignancies. | Expert opinion on investigational drugs 20100801 |
Src family kinase inhibitor Saracatinib (AZD0530) impairs oxaliplatin uptake in colorectal cancer cells and blocks organic cation transporters. | Cancer research 20100715 |
Effects of the Src inhibitor saracatinib (AZD0530) on renal function in healthy subjects. | Anticancer research 20100701 |
Emerging targets in osteoporosis disease modification. | Journal of medicinal chemistry 20100610 |
A novel bile acid-activated vitamin D receptor signaling in human hepatocytes. | Molecular endocrinology (Baltimore, Md.) 20100601 |
Effect of the specific Src family kinase inhibitor saracatinib on osteolytic lesions using the PC-3 bone model. | Molecular cancer therapeutics 20100601 |
Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: a randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial. | Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 20100301 |
Src tyrosine kinase regulates adhesion and chemotaxis in Waldenstrom macroglobulinemia. | Clinical cancer research : an official journal of the American Association for Cancer Research 20091001 |
Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090615 |
Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer. | The Journal of clinical endocrinology and metabolism 20090601 |
Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. | Molecular oncology 20090601 |
Combined Src and aromatase inhibition impairs human breast cancer growth in vivo and bypass pathways are activated in AZD0530-resistant tumors. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090515 |
Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells. | Breast cancer research and treatment 20090501 |
Structure-based virtual screening of Src kinase inhibitors. | Bioorganic & medicinal chemistry 20090415 |
The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. | Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20090401 |
The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts. | Molecular cancer research : MCR 20090401 |
Src inhibitors in early breast cancer: a methodology, feasibility and variability study. | Breast cancer research and treatment 20090301 |
Quantification of focal adhesion kinase activation loop phosphorylation as a biomarker of Src activity. | Molecular pharmacology 20090301 |
A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study. | Anti-cancer drugs 20090301 |
A novel Src kinase inhibitor reduces tumour formation in a skin carcinogenesis model. | Carcinogenesis 20090201 |
Src as a therapeutic target in men with prostate cancer and bone metastases. | BJU international 20090201 |
Improved response by co-targeting EGFR/EGFRvIII and Src family kinases in human cancer cells. | Cancer investigation 20090201 |
Activation of Src and Src-associated signaling pathways in relation to hypoxia in human cancer xenograft models. | International journal of cancer 20090115 |
Aberrant activation of androgen receptor in a new neuropeptide-autocrine model of androgen-insensitive prostate cancer. | Cancer research 20090101 |
The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines. | BMC cancer 20090101 |
Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. | Oncogene 20081023 |
Research provides new hope for tamoxifen-resistant breast cancer patients. | Women's health (London, England) 20080301 |
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics. | Nature chemical biology 20070401 |
Cooperative action of tamoxifen and c-Src inhibition in preventing the growth of estrogen receptor-positive human breast cancer cells. | Molecular cancer therapeutics 20061201 |
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. | Journal of medicinal chemistry 20061102 |
Clinical development of SRC tyrosine kinase inhibitors in lung cancer. | Clinical lung cancer 20060501 |