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CAS No. 379231-04-6
Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Selleck's Saracatinib (AZD0530) has been cited by 209 publications
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|Description||Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.|
|Features||The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.|
Saracatinib also potently inhibits other Src tyrosine kinase family members including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck with IC50 from 4-10 nM. Saracatinib sensitively inhibits Src Y530F NIH 3T3 with IC50 of 80 nM. Saracatinib signiﬁcantly impairs the invasion of HT1080 cells through a 3-dimensional collagen matrix and completely inhibits EGF-induced cell scattering in NBT-II bladder cancer cells.  Saracatinib potent inhibits Src activation in DU145 and PC3 cells, which through inhibition of Y419 phosphorylation. Saracatinib inhibits the growth of prostate cancer including PC3, DU145, CWR22Rv1 and LNCaP, while Saracatinib shows low activity in LAPC-4, PZ-HPV7 and RWPE-1 cells. Saracatinib induces cell cycle arrest at G1/S but not caspase 3 cleavages. Saracatinib also significantly inhibits DU145 and PC3 migration in the Boyden chamber.  Saracatinib gives a potent and sustained blockage of AKT and enhances the sensitivity to irradiation in A549 and Calu-6 cells.  Saracatinib inhibits osteoclast in activity, resorption and formation. Saracatinib also reversibly prevents osteoclast precursor migration. 
Saracatinib shows great tumor growth inhibition in Src3T3 allografts and a moderate growth delay in Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts.  Saracatinib shows great antitumor activity in orthotopic DU145 xenograft mice at a dose of 25mg/kg (orally administered, daily). 
Kinase Assay:IC50 of tyrosine kinase activity is measured by an enzyme-linked immunosorbent assay (ELISA) with recombinant catalytic domains of a panel of receptor and non-receptor tyrosine kinases (in some cases only part of the catalytic domain is used). Saracatinib dose ranges from 0.001-10 mM. Speciﬁcity assays against a panel of serine/threonine kinases are performed using a ﬁlter capture assay with 32P. Brieﬂy, multidrop 384 plates containing 0.5 μL Saracatinib or controls (DMSO) alone or pH 3.0 buffer controls) are incubated with 15 μL of enzyme plus peptide/protein substrate for 5 min before the reaction is initiated by the addition of 10 μL of 20 mM Mg-ATP. For all enzymes the ﬁnal concentration is approximated to the Michaelis constant (Km). Assays are carried out for 30min at room temperature before termination by the addition of 5 μL orthophosphoric acid. After mixing, the well contents are harvested onto a P81 Uniﬁlter plate, using orthophosphoric acid as the wash buffer. Then IC50 is calculated.
-  Chang YM, Oncogene, 2008, 27(49), 6365-6375.
-  Green TP, et al. Mol Oncol, 2009, 3(3), 248-261.
-  Purnell PR, et al. J Thorac Oncol, 2009, 4(4), 448-454.
|In vitro||DMSO||35 mg/mL warmed (64.57 mM)|
|Ethanol||31 mg/mL (57.19 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04598919||Recruiting||Drug: Saracatinab|Drug: Placebo||Idiopathic Pulmonary Fibrosis (IPF)||National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Science (NCATS)||November 12 2020||Phase 1|Phase 2|
|NCT04307953||Recruiting||Drug: AZD0530 Difumarate|Drug: Matching placebo||Fibrodysplasia Ossificans Progressiva||VU University Medical Center|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative||August 5 2020||Phase 2|
|NCT02085603||Completed||Drug: Saracatinib|Drug: Placebo||Cancer||Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca||March 2014||Phase 2|
|NCT01864655||Completed||Drug: saracatinib|Drug: Placebo||Alzheimer''s Disease||Stephen M. Strittmatter|Yale University||July 2013||Phase 1|
|NCT01000896||Withdrawn||Drug: AZD0530|Drug: Carboplatin|Drug: paclitaxel||Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer||AstraZeneca||January 2010||Phase 1|
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Frequently Asked Questions
What is the half-life of Saracatinib?
Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long