GW2580 870483-87-7

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Molecular Weight:

366.41 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.


Biological Activity


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.


GW2580 (dosed orally at 40 mg/kg 0.5 h before the CSF-1-priming dose)
blocks the ability of exogenous CSF-1 to increase LPS-induced TNF-α
production in mice by 63%. When given to mice before CSF-1 priming,
GW2580 completely blocks the ability of CSF-1 to prime the mouse for
increased IL-6 production. GW2580 (80 mg/kg p.o.) completely inhibits
the growth of CSF-1-dependent M-NFS-60 tumor cells in the peritoneal
cavity.


GW2580 (80 mg/kg) dosed orally twice a day the week before
thioglycolate injection and for the 4-day period after thioglycolate
injection, diminishes the accumulation of macrophages in the peritoneal
cavity after thioglycolate injection (by 45%). In a
21-day adjuvant arthritis model, GW2580 (50 mg/kg) dosed twice a day
from days 0 to 21, 7 to 21, or 14 to 21 inhibits joint connective tissue
and bone destruction.


Gw2580 (160 mg/kg) induces a more than 2-fold reduction of total CD45+ CD11b+ myeloid cells, CD11b+ F4/80+ TAMs, and CD11b+ Gr-1+ MDSCs in implanted 3LL lung tumor, through inhibiting tumor recruitment
of myeloid cells from peripheral blood. GW2580 (80 mg/kg) treatment is
able to suppress Vegf-a (by 35%) and Mmp9 (by 70%) expression, as well
as tumor vascular density (CD31 staining).


Combination therapy with
GW2580 and an anti-VEGFR-2 antibody results in synergistic tumor growth
reduction. DC101 alone reduces tumor growth by 35%, the combination of
DC101 and GW2580 results in an apparent synergistic tumor growth
reduction of approximately 70%.

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Product Categories : Protein Tyrosine Kinase > CSF-1R Inhibitor