Name: SD-208
Price: 365.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SD-208 Description:EC50: SD-208 inhibits the growth inhibition of TGF-β–sensitive CCL64 cells at an EC50 of 0.1 μmol/L .The cytokine transforming growth factor (TGF)-β has become a major target for the experimental treatment of human malignant gliomas. SD-208, a novel transforming growth factor β receptor I kinase inhibitor, inhibits growth and invasiveness and enhances immunogenicity of murine and human Glioma cells both in vitro and in vivo. In vitro: SD-208 inhibits the growth inhibition of TGF-β–sensitive CCL64 cells mediated by recombinant TGF-β1 or TGF-β2 or of TGF-β–containing glioma cell supernatant at an EC50 of 0.1 μmol/L. SD-208 also blocks autocrine and paracrine TGF-β signaling in glioma cells as detected by the phosphorylation of Smad2 or TGF-β reporter assays and strongly inhibits constitutive and TGF-β–evoked migration and invasion, but not viability or proliferation. Moreover, SD-208 restores the lytic activity of polyclonal natural killer cells against glioma cells in the presence of recombinant TGF-β or of TGF-β–containing glioma cell supernatant. [1]. In vivo: The oral bioavailability of SD-208 was verified by demonstrating the inhibition of TGF-β–induced Smad phosphorylation in spleen and brain. Systemic SD-208 treatment initiated 3 days after the implantation of SMA-560 cells into the brains of syngeneic VM/Dk mice prolongs their median survival from 18.6 to 25.1 days. Histologic analysis revealed no difference in blood vessel formation, proliferation, or apoptosis. However, animals responding to SD-208 showed an increased tumor infiltration by natural killer cells, CD8 T cells, and macrophages. These data define TGF-β receptor I kinase inhibitors such as SD-208 as promising novel agents for the treatment of human malignant glioma and other conditions associated with pathological TGF-β activity [1]. Clinical trial: Up to now, SD-208 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    SD 208; SD208; 2-(5-chloro-2-fluorophenyl)-N-pyridin-4-ylpteridin-4-amine
    
    CAS Number
    
    627536-09-8
    
    Molecular Formula
    
    C17H10ClFN6
    
    Molecular Weight
    
    352.75
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥8.95 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

SD-208

SD-208

Background

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