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GW2580 870483-87-7

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Synonyms ：
Appearance ：
Chemical Formula ：
C20H22N4O3
Solubility ：
Molecular Weight ：
366.41
Storage and Stability ：
in stock
CAS No. ：
870483-87-7
Purity ：
98%+
Introduction
GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

GW2580 completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 inhibits the growth of CSF-1 stimulated M-NFS-60 myeloid tumor cells, serum stimulated NSO myeloid tumor cells, CSF-1 stimulated freshly isolated human monocytes, and VEGF stimulated human umbilical vein vascular endothelial cells with IC50 of 0.33, 13.5, 0.47 and 12 μM, respectively. 1 μM GW2580 completely inhibits CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibits bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC50 of approximately 10 nM. GW2580 also inhibits TRKA activity with IC50 of 0.88 μM.

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