Name: GW2580
Price: 204.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GW2580 is a selective and orally bioavailable inhibitor of Colony-stimulating-factor-1 receptor (CSF-1R) with IC50 value of 30nM [1]
    GW2580 has been demonstrated to be an extremely selective inhibitor for CSF-1R and has been hypothesized to bind to the DFG-out mode of CSF-1R, which might lock it into an inactive conformation [2] GW2580 has shown to inhibit epithelial cell-associated CSF-1 signaling, reduce Gr-1+ CD11b+ myeloid-derived suppressor cells (MDSCs) expansion, and alleviate the immune-suppressive microenvironment [3]. In addition, GW2580 suppressed IL-10 secretion in human glioblastoma cell line T98G [4].
    
    [1] Conway JG1, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM, Johnson JH, Frick L, Lin MH, Depee S, Tadepalli S,Votta B, James I, Fuller K, Chambers TJ, Kull FC, Chamberlain SD, Hutchins JT. Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83.
    [2] Garcia AJ1, Ruscetti M, Arenzana TL, Tran LM, Bianci-Frias D, Sybert E, Priceman SJ, Wu L, Nelson PS, Smale ST, Wu H. Pten Null Prostate Epithelium Promotes Localized Myeloid-Derived Suppressor Cell Expansion and Immune Suppression during Tumor Initiation and Progression. Mol Cell Biol. 2014 Jun;34(11):2017-28.
    [3] Kitagawa D1, Gouda M, Kirii Y, Sugiyama N, Ishihama Y, Fujii I, Narumi Y, Akita K, Yokota K. Characterization of kinase inhibitors using different phosphorylation states of colony stimulating factor-1 receptor tyrosine kinase. J Biochem. 2012 Jan;151(1):47-55.
    [4] Komohara Y1, Horlad H, Ohnishi K, Fujiwara Y, Bai B, Nakagawa T, Suzu S, Nakamura H, Kuratsu J, Takeya M. Importance of direct macrophage-tumor cell interaction on progression of human glioma. Cancer Sci. 2012 Dec;103(12):2165-72.
- Properties
  - Alternative Name
    
    5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine
    
    CAS Number
    
    870483-87-7
    
    Molecular Formula
    
    C20H22N4O3
    
    Molecular Weight
    
    366.41
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥36.6 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jiqing Tang, Jun Liu, et al. "Konjac Glucomannan Oligosaccharides Prevent Intestinal Inflammation Through SIGNR1‐Mediated Regulation of Alternatively Activated Macrophages." Mol Nutr Food Res. 2021 Oct;65(20):e2001010. PMID:34390195
    2. Ramadurgum P, Woodard DR, et al. "Simultaneous Control of Endogenous and User-Defined Genetic Pathways Using Unique ecDHFR Pharmacological Chaperones." Cell Chem Biol. 2020;27(5):622-634.e6. PMID:32330442
    3. Alexandria N. Hughes, Bruce Appel. "Microglia phagocytose myelin sheaths to modify developmental myelination." Nature Neuroscience (2020); 06 July 2020.
    4. Green LA, Nebiolo JC, et al. "Microglia exit the CNS in spinal root avulsion." PLoS Biol. 2019 Feb 22;17(2):e3000159. PMID:3000159

GW2580

GW2580

Background

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