Name: AZD4547
Price: 230.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    AZD4547 is a potent, specific, orally bioavailable fibroblast growth factors receptor (FGFR) tyrosine kinase inhibitor. It inhibits FGFR1, FGFR2, and FGFR3 with IC50 values of 12, 2 and 40 nM, respectively. AZD4547 has also been reported to block FGFR1, FGFR2, and FGFR3 autophosphorylation with IC50 values of 0.2, 2.5, and 1.8 nM, respectively [1].AZD4547 has been demonstrated to inhibit cell proliferation and inhibit FGFRs and their downstream markers including PLCg and FRS2 phosphorylation in breast cell line Sum52-PE (expressing wild-type FGFR2), multiple myeloma line KMS11 (expressing Y373C mutated FGFR3 protein) and acute myeloid leukemia cell line KG1a (expressing wild-type FGFR1) [1]. Anti-carcinoma effect of AZD4547 has been observed in lung cancer xeonograft mice orally treated with AZD4547. This effect is believed to be via the specifically inhibition of the activity of FGFR but not kinase insert domain receptor (KDR)[1].
    
    [1] Gavine PR1,?Mooney L,?Kilgour E,?Thomas AP,?Al-Kadhimi K,?Beck S,?Rooney C,?Coleman T,?Baker D,?Mellor MJ,?Brooks AN,?Klinowska T. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res.?2012 Apr 15;72(8):2045-56.
- Properties
  - Alternative Name
    
    AZD 4547;AZD-4547; N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide
    
    CAS Number
    
    1035270-39-3
    
    Molecular Formula
    
    C26H33N5O3
    
    Molecular Weight
    
    463.57
    
    Appearance
    
    A solid
    
    Purity
    
    99.34%
    
    Solubility
    
    ≥23.2 mg/mL in DMSO; insoluble in H2O; ≥6.33 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Hugh A. Nicholson, Lynne Sawers, et al. "Fibroblast growth factor signalling influences homologous recombination-mediated DNA damage repair to promote drug resistance in ovarian cancer." Br J Cancer. 2022 Oct;127(7):1340-1351. PMID: 35778553
    2. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID: 32160544
    3. Else Driehuis. "Organoids as a tool for fundamental and translational oncology research: Can organoids guide clinical decision making?" Universiteit Utrecht. 2019.
    4. Driehuis E, Kolders S, et al. "Oral Mucosal Organoids as a Potential Platform for Personalized Cancer Therapy." Cancer Discov. 2019 Jul;9(7):852-871. PMID: 31053628

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AZD4547

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