CFMS kinase/CSF-1R inhibitor,selective and ATP-competitive
CAS：870483-87-7
分子式：C20H22N4O3
分子量：366.41
纯度：98%
存储：Store at -20°C

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].

参考文献:
[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.