379231-04-6 | Saracatinib

Packsize	Purity	Availability	Price	Discounted Price
5mg	≥90%	in stock	$40.00	$28.00
10mg	98%	in stock	$44.00	$31.00
50mg	≥90%	in stock	$196.00	$137.00
100mg	98%	in stock	$330.00	$231.00
250mg	98%	in stock	$620.00	$434.00

Description

• Catalog Number: AB52353
• Chemical Name: Saracatinib
• CAS Number: 379231-04-6
• Molecular Formula: C27H32ClN5O5
• Molecular Weight: 542.0265
• MDL Number: MFCD09832698
• SMILES: CN1CCN(CC1)CCOc1cc(OC2CCOCC2)c2c(c1)ncnc2Nc1c(Cl)ccc2c1OCO2

Computed Properties

• Complexity: 743
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 38
• Hydrogen Bond Acceptor Count: 10
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 8
• XLogP3: 4.1

Literature

• 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