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Saracatinib (AZD0530)

Catalog No. S1006 5 5 8 Customer Review(s) Product Citations9 Product Citation(s)
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Saracatinib (AZD0530) Chemical Structure

Bio Information

Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively. Saracatinib (AZD0530) a novel anilino quinazoline. AZD0530(Saracatinib) is highly selective for Src and Abl kinases against a large range of tyrosine and serine- threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). Saracatinib (AZD0530) exerts its activity through ATP competitive and reversible inhibition of the target enzyme. Saracatinib (AZD0530) potently inhibited the in vitro proliferation of Src3T3 mouse fibroblasts and demonstrated 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 (AZD0530) was observed with IC50 values of 0.2~0.7 µM. In 3-day MTS cell proliferation assays, Saracatinib (AZD0530) inhibited in vitro proliferation of the Bcr–Abl-driven human leukemia cell line K562 with an IC50 of 0.22 µM. In a head-to-head assay measuring EGFR phosphorylation in KB cells, Saracatinib (AZD0530) exhibited an IC50 of 1.25 mM compared with 11 nM for gefitinib. [1][2]

References:

[2] Proc Amer Assoc Cancer Res. 2005;Volume 46

[1] MOLECULAR ONCOLOGY 2009;3:248–261

Chemical Information

Molecular Weight (WM): 542.03
Formula:

C27H32ClN5O5
Solubility(R.T.:25°C): DMSO 108mg/mL 
Water <1mg/mL 
Ethanol 108mg/mL 

Quality Control

View current batch:
H-NMR HPLC H-NMR HPLC H-NMR HPLC H-NMR HPLC

Research Area

Angiogenesis >> Src >> Src Inhibitors

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Related Antibodies

Information  
Reactivity: 薛亚红

Saracatinib (AZD0530) has been referenced in 9 publications.

Hepatitis B virus large surface antigen promotes liver carcinogenesis by activating the Src/PI3K/Akt pathway.
Saracatinib (AZD0530) is a potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo.
A novel bile acid-activated vitamin D receptor signaling in human hepatocytes.
Small molecule inhibition of the steroid receptor coactivators, SRC-3 and SRC-1.
Targeting cell spreading: a method of sensitizing metastatic tumor cells to TRAIL-induced apoptosis.
Temozolomide modifies caveolin-2 expression in experimental malignant gliomas in vitro and in vivo.
Enhancing CHK1 inhibitor lethality in glioblastoma.
Simultaneous exposure of transformed cells to SRC family inhibitors and CHK1 inhibitors causes cell death.
Translation of a Tumor Microenvironment Mimicking 3D Tumor Growth Co-culture Assay Platform to High-Content Screening.

We have 8 customer reviews of Saracatinib (AZD0530).

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Average Customer Review

(8 customer reviews)

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  • ;Cancer Res, 2011, 71(24), 7547-57
    Saracatinib (AZD0530) purchased from Selleck


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  • ;J Biomol Screen, 2013, 18(1), 54-66
    Saracatinib (AZD0530) purchased from Selleck


  • Click to enlarge

  • ;J Biomol Screen, 2013, 18(1), 54-66
    Saracatinib (AZD0530) purchased from Selleck


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  • ;Translational Oncology, 2011, 4, 92-100
    Saracatinib (AZD0530) purchased from Selleck


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  • ;Mol Cancer Res, 2011, 9, 249-258
    Saracatinib (AZD0530) purchased from Selleck


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  • ;Cancer Biol Ther, 2011, 12(3), 215-28
    Saracatinib (AZD0530) purchased from Selleck


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  • ;Cancer Res, 2011, 71(24), 7547-57
    Saracatinib (AZD0530) purchased from Selleck


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  • ;Dr Shuxin Han of Kent State University
    Saracatinib (AZD0530) purchased from Selleck

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;Cancer Res, 2011, 71(24), 7547-57


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;J Biomol Screen, 2013, 18(1), 54-66

+ See All 8 Customer Reviews of Saracatinib (AZD0530)

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