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379231-04-6,MFCD09832698
Catalog No.:AA0039MT

379231-04-6 | Saracatinib

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5mg
≥90%
in stock  
$45.00   $31.00
- +
10mg
98%
in stock  
$47.00   $33.00
- +
50mg
≥90%
in stock  
$218.00   $152.00
- +
100mg
98%
in stock  
$377.00   $264.00
- +
250mg
98%
in stock  
$700.00   $490.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA0039MT
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
Properties
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  

Downstream Synthesis Route
5464-12-0    379229-54-6   
saracatinib 

[1]JournalofMedicinalChemistry,2006,vol.49,p.6465-6488

[2]Patent:CN107814793,2018,A.Locationinpatent:Paragraph0018;0021

[3]Patent:CN107987064,2018,A.Locationinpatent:Paragraph0013;0014;0015

[1]Hennequin,LaurentF.;Allen,Jack;Breed,Jason;Curwen,Jon;Fennell,Michael;Green,TimP.;Lambert-VanDerBrempt,Christine;Morgentin,Rémy;Norman,RichardA.;Olivier,Annie;Otterbein,Ludovic;Plé,PatrickA.;Warin,Nicolas;Costello,Gerard[JournalofMedicinalChemistry,2006,vol.49,#22,p.6465-6488]

[1]Hennequin,LaurentF.;Allen,Jack;Breed,Jason;Curwen,Jon;Fennell,Michael;Green,TimP.;Lambert-VanDerBrempt,Christine;Morgentin,Rémy;Norman,RichardA.;Olivier,Annie;Otterbein,Ludovic;Plé,PatrickA.;Warin,Nicolas;Costello,Gerard[JournalofMedicinalChemistry,2006,vol.49,#22,p.6465-6488]

[1]Hennequin,LaurentF.;Allen,Jack;Breed,Jason;Curwen,Jon;Fennell,Michael;Green,TimP.;Lambert-VanDerBrempt,Christine;Morgentin,Rémy;Norman,RichardA.;Olivier,Annie;Otterbein,Ludovic;Plé,PatrickA.;Warin,Nicolas;Costello,Gerard[JournalofMedicinalChemistry,2006,vol.49,#22,p.6465-6488]

[1]Hennequin,LaurentF.;Allen,Jack;Breed,Jason;Curwen,Jon;Fennell,Michael;Green,TimP.;Lambert-VanDerBrempt,Christine;Morgentin,Rémy;Norman,RichardA.;Olivier,Annie;Otterbein,Ludovic;Plé,PatrickA.;Warin,Nicolas;Costello,Gerard[JournalofMedicinalChemistry,2006,vol.49,#22,p.6465-6488]

Literature

Title: Cytochrome P450 Mediated Bioactivation of Saracatinib.

Journal: Chemical research in toxicology 20161121

Title: Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.

Journal: ACS medicinal chemistry letters 20150709

Title: Lipopolysaccharide-induced caveolin-1 phosphorylation-dependent increase in transcellular permeability precedes the increase in paracellular permeability.

Journal: Drug design, development and therapy 20150101

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo.

Journal: International journal of cancer 20130101

Title: 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.

Journal: Investigational new drugs 20121001

Title: Src-signaling interference impairs the dissemination of blood-borne tumor cells.

Journal: Cell and tissue research 20120801

Title: Antitumor activity of Src inhibitor saracatinib (AZD-0530) in preclinical models of biliary tract carcinomas.

Journal: Molecular cancer therapeutics 20120701

Title: False-negative MRI biomarkers of tumour response to targeted cancer therapeutics.

Journal: British journal of cancer 20120605

Title: 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.

Journal: Investigational new drugs 20120601

Title: Simultaneous targeting of Src kinase and receptor tyrosine kinase results in synergistic inhibition of renal cell carcinoma proliferation and migration.

Journal: International journal of cancer 20120601

Title: Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours.

Journal: British journal of cancer 20120522

Title: Role of Src in breast cancer cell migration and invasion in a breast cell/bone-derived cell microenvironment.

Journal: Breast cancer research and treatment 20120501

Title: Distinct effects of saracatinib on memory CD8+ T cell differentiation.

Journal: Journal of immunology (Baltimore, Md. : 1950) 20120501

Title: Common PIK3CA mutants and a novel 3' UTR mutation are associated with increased sensitivity to saracatinib.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120501

Title: A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.

Journal: Investigational new drugs 20120401

Title: Effects of Src kinase inhibition by saracatinib (AZD0530) on bone turnover in advanced malignancy in a Phase I study.

Journal: Bone 20120401

Title: An update on dual Src/Abl inhibitors.

Journal: Future medicinal chemistry 20120401

Title: TRAF6 inhibits proangiogenic signals in endothelial cells and regulates the expression of vascular endothelial growth factor.

Journal: Biochemical and biophysical research communications 20120302

Title: WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors.

Journal: Laboratory investigation; a journal of technical methods and pathology 20120301

Title: Modulation of epithelial tight junctions by TGF-beta 3 in cultured oral epithelial cells.

Journal: Australian dental journal 20120301

Title: In silico investigation of potential SRC kinase ligands from traditional Chinese medicine.

Journal: PloS one 20120101

Title: Traditional Chinese medicine as dual guardians against hypertension and cancer?

Journal: Journal of biomolecular structure & dynamics 20120101

Title: Hepatitis B virus large surface antigen promotes liver carcinogenesis by activating the Src/PI3K/Akt pathway.

Journal: Cancer research 20111215

Title: Phase II trial of saracatinib (AZD0530), an oral SRC-inhibitor for the treatment of patients with hormone receptor-negative metastatic breast cancer.

Journal: Clinical breast cancer 20111001

Title: Expression and functional role of CRIPTO-1 in cutaneous melanoma.

Journal: British journal of cancer 20110927

Title: Simultaneous exposure of transformed cells to SRC family inhibitors and CHK1 inhibitors causes cell death.

Journal: Cancer biology & therapy 20110801

Title: Combined Src and ER blockade impairs human breast cancer proliferation in vitro and in vivo.

Journal: Breast cancer research and treatment 20110701

Title: Current status of SRC inhibitors in solid tumor malignancies.

Journal: The oncologist 20110501

Title: Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors.

Journal: Bioorganic & medicinal chemistry 20110415

Title: Osteoporosis: now and the future.

Journal: Lancet (London, England) 20110409

Title: Phase II study of saracatinib (AZD0530) for patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC).

Journal: Anticancer research 20110101

Title: Impact of the Src inhibitor saracatinib on the metastatic phenotype of a fibrosarcoma (KHT) tumor model.

Journal: Anticancer research 20101101

Title: Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20101001

Title: [SRC kinases in tumor therapy].

Journal: Medizinische Klinik (Munich, Germany : 1983) 20101001

Title: Gene array and fluorescence in situ hybridization biomarkers of activity of saracatinib (AZD0530), a Src inhibitor, in a preclinical model of colorectal cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20100815

Title: Novel dual Src/Abl inhibitors for hematologic and solid malignancies.

Journal: Expert opinion on investigational drugs 20100801

Title: Src family kinase inhibitor Saracatinib (AZD0530) impairs oxaliplatin uptake in colorectal cancer cells and blocks organic cation transporters.

Journal: Cancer research 20100715

Title: Effects of the Src inhibitor saracatinib (AZD0530) on renal function in healthy subjects.

Journal: Anticancer research 20100701

Title: Emerging targets in osteoporosis disease modification.

Journal: Journal of medicinal chemistry 20100610

Title: A novel bile acid-activated vitamin D receptor signaling in human hepatocytes.

Journal: Molecular endocrinology (Baltimore, Md.) 20100601

Title: Effect of the specific Src family kinase inhibitor saracatinib on osteolytic lesions using the PC-3 bone model.

Journal: Molecular cancer therapeutics 20100601

Title: 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: Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 20100301

Title: Src tyrosine kinase regulates adhesion and chemotaxis in Waldenstrom macroglobulinemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20091001

Title: Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090615

Title: Inhibition of Src with AZD0530 reveals the Src-Focal Adhesion kinase complex as a novel therapeutic target in papillary and anaplastic thyroid cancer.

Journal: The Journal of clinical endocrinology and metabolism 20090601

Title: Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.

Journal: Molecular oncology 20090601

Title: Combined Src and aromatase inhibition impairs human breast cancer growth in vivo and bypass pathways are activated in AZD0530-resistant tumors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090515

Title: Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells.

Journal: Breast cancer research and treatment 20090501

Title: Structure-based virtual screening of Src kinase inhibitors.

Journal: Bioorganic & medicinal chemistry 20090415

Title: The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20090401

Title: The Src inhibitor AZD0530 reversibly inhibits the formation and activity of human osteoclasts.

Journal: Molecular cancer research : MCR 20090401

Title: Src inhibitors in early breast cancer: a methodology, feasibility and variability study.

Journal: Breast cancer research and treatment 20090301

Title: Quantification of focal adhesion kinase activation loop phosphorylation as a biomarker of Src activity.

Journal: Molecular pharmacology 20090301

Title: A phase II trial of the Src-kinase inhibitor AZD0530 in patients with advanced castration-resistant prostate cancer: a California Cancer Consortium study.

Journal: Anti-cancer drugs 20090301

Title: A novel Src kinase inhibitor reduces tumour formation in a skin carcinogenesis model.

Journal: Carcinogenesis 20090201

Title: Src as a therapeutic target in men with prostate cancer and bone metastases.

Journal: BJU international 20090201

Title: Improved response by co-targeting EGFR/EGFRvIII and Src family kinases in human cancer cells.

Journal: Cancer investigation 20090201

Title: Activation of Src and Src-associated signaling pathways in relation to hypoxia in human cancer xenograft models.

Journal: International journal of cancer 20090115

Title: Aberrant activation of androgen receptor in a new neuropeptide-autocrine model of androgen-insensitive prostate cancer.

Journal: Cancer research 20090101

Title: The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines.

Journal: BMC cancer 20090101

Title: Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530.

Journal: Oncogene 20081023

Title: Research provides new hope for tamoxifen-resistant breast cancer patients.

Journal: Women's health (London, England) 20080301

Title: Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.

Journal: Nature chemical biology 20070401

Title: Cooperative action of tamoxifen and c-Src inhibition in preventing the growth of estrogen receptor-positive human breast cancer cells.

Journal: Molecular cancer therapeutics 20061201

Title: 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: Journal of medicinal chemistry 20061102

Title: Clinical development of SRC tyrosine kinase inhibitors in lung cancer.

Journal: Clinical lung cancer 20060501

Title: Green TP, et al. Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol, 2009, 3(3), 248-261.

Title: Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398.

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