GW2580 |
| Catalog No.GC17286 |
CFMS kinase/CSF-1R inhibitor,selective and ATP-competitive
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 870483-87-7
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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