Saracatinib (AZD0530)

Saracatinib (AZD0530)

Catalog Number:
L002368385APE
Mfr. No.:
APE-A2133
Price:
$196
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      • Overview
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          Background

          Saracatinib (AZD0530) is a novel, potent Src family kinase (SFK)/Abl dual-kinase inhibitor with IC50 value of 2.7 nM [1].Saracatinib has been reported to inhibit Src activation in DU145 and PC3 cell lines (prostate cancer cell lines). Both of c-Myc and cyclin D1 expression are decreased by Saracatinib. Saracatinib can inhibit the ERK1/2 and GSK3b phosphorylation as well as decrease β-catenin level in cells. Saracatinib inhibits the prostate tumor cell growth by inducing cycle arrest at G1/S phase. Saracatinib dose-dependently blocks cell migration in DU145 and PC3 cell lines [1].In DU145 implanted orthotopic SCID mice model, treatment with Saracatinib has been demonstrated to down-regulate the Src expression as well as suppress the tumor size [1].

          [1] Chang YM1, Bai L, Liu S, Yang JC, Kung HJ, Evans CP. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene. 2008 Oct 23;27(49):6365-75.

      • Properties
        • Alternative Name
          N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine
          CAS Number
          379231-04-6
          Molecular Formula
          C27H32ClN5O5
          Molecular Weight
          542.03
          Purity
          98.35%
          Solubility
          ≥27.1 mg/mL in DMSO; insoluble in EtOH; ≥2.36 mg/mL in H2O with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Xu Wang, Xinfang Yu, et al. "Expanding anti-CD38 immunotherapy for lymphoid malignancies." J Exp Clin Cancer Res. 2022 Jun 28;41(1):210 PMID: 35765110
          2. Liao X, Song G, et al. "Oxaliplatin resistance is enhanced by saracatinib via upregulation Wnt-ABCG1 signaling in hepatocellular carcinoma." BMC Cancer. 2020;20(1):31. PMID: 31931755
          3. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID: 31862381
          4. Alzubi MA, Turner TH, et al. "Separation of breast cancer and organ microenvironment transcriptomes in metastases." Breast Cancer Res. 2019 Mar 6;21(1):36. PMID: 30841919
          5. Nakachi I, Helfrich BA, et al. "PTTG1 Levels Are Predictive of Saracatinib Sensitivity in Ovarian Cancer Cell Lines." Clin Transl Sci. 2016 Dec;9(6):293-301. PMID: 27766744
          6. Diao Y, Ma X, et al. "Dasatinib promotes paclitaxel-induced necroptosis in lung adenocarcinoma with phosphorylated caspase-8 by c-Src." Cancer Lett. 2016 May 16. PMID: 27195913

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