PD 173074

- Overview
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    Background
    
    PD173074 is a poten and selective fibroblast growth factor receptor (FGFR) inhibitor. Fibroblast growth factor-2 is reported to be able to induce proliferation and chemoresistance in Small cell lung cancer (SCLC) cells.
    In vitro: PD173074 was found to block H-510 and H-69 SCLC proliferation and clonogenic growth in a dose-dependent fashion and prevent FGF-2-induced chemoresistance as well. These effects correlate with the inhibition of both FGFR1 and FGFR2 transphosphorylation. In addition, PD173074 showed a high degree of selectivity for FGFR tyrosine kinase [2].
    In vivo: In the H-510 xenograft mouse model, tumor growth was significanlty improved similar to that seen with single-agent cisplatin administration. Accordingly, PD173074 treatment resulted in significanlty prolonged median survival when compared with that of control sham-treated animals. More dramatically, PD173074 also induced complete responses lasting >6 months in 50% of in mice H-69 xenografts [2].
    Clinical trial: PD173074 is still in the preclinical development stage, and no clinical data are available currently.
    
    [1] Pardo OE, Latigo J, Jeffery RE, Nye E, Poulsom R, Spencer-Dene B, Lemoine NR, Stamp GW, Aboagye EO, Seckl MJ. The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo. Cancer Res. 2009 Nov 15;69(22):8645-51.
    [2] Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J. 1998 Oct 15;17(20):5896-904.
- Properties
  - Alternative Name
    
    PD 173074,PD-173074; 1-tert-butyl-3-[2-[4-(diethylamino)butylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea
    
    CAS Number
    
    219580-11-7
    
    Molecular Formula
    
    C28H41N7O3
    
    Molecular Weight
    
    523.67
    
    Appearance
    
    A solid
    
    Purity
    
    99.22%
    
    Solubility
    
    ≥26.18 mg/mL in DMSO; insoluble in H2O; ≥108.4 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at 4°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. Chen P, Zhang H, et al. "Basic Fibroblast Growth Factor Reduces Permeability and Apoptosis of Human Brain Microvascular Endothelial Cells in Response to Oxygen and Glucose Deprivation Followed by Reoxygenation via the Fibroblast Growth Factor Receptor 1 (FGFR1)/ERK Pathway." Med Sci Monit. 2019 Sep 25;25:7191-7201. PMID:31551405

PD 173074

Background

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