Molecular Formula | C20H22N4O3 |
Molar Mass | 366.41 |
Solubility | DMSO: soluble10mg/mL, clear (warmed) |
Appearance | powder |
Color | white to beige |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
In vitro study | 0.06 μm GW2580 completely inhibits human CFMS kinase in vitro. GW2580 inhibits the growth of CSF-1-stimulated M-NFS-60 myeloma cells, serum-stimulated NSO myeloma cells, CSF-1-stimulated freshly isolated human monocytes, and VEGF-stimulated human umbilical vein endothelial cells, the IC50 was 0.33, 13.5, 0.47 and 12 μm, respectively. 1 μm GW2580 acted on the culture medium of human osteoclast, rat skull, and Rat fetal long bone, completely inhibited the growth of CSF-1-induced mouse M-NFS-60 bone marrow cells and human monocytes, and completely inhibit bone degeneration. GW2580 acts on RAW264.7 mouse macrophages to inhibit CSF1R phosphorylation, and the IC50 is about 10 nM. GW2580 also inhibited TRKA activity with an IC50 of 0.88 μm. |
In vivo study | GW2580 (treated mice orally at a dose of 40 mg/kg for 0.5 hours) inhibited the ability of exogenous CSF-1 to promote LPS-induced TNF-α production by 63%. Treatment of mice with GW2580 followed by treatment with CSF-1 completely inhibited the ability of CSF-1 to increase IL-6 production in mice. GW2580(80 mg/kg P. O.) completely inhibited the growth of intraperitoneal CSF-1-dependent M-NFS-60 tumor cells. Treatment with GW2580(80 mg/kg) orally twice daily for one week followed by thioglycolic acid injection for 4 days reduced macrophage volume by 45%. The adjuvant arthritis model was treated with GW2580(50 mg/kg) twice daily for 21 days on a schedule of 0 to 21 days, 7 to 21 days, or 14 to 21 days, inhibition of joint connective tissue and bone destruction. GW2580(160 mg/kg) treatment of transplanted 3LL lung tumors induced total CD45 |
Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.729 ml | 13.646 ml | 27.292 ml |
5 mM | 0.546 ml | 2.729 ml | 5.458 ml |
10 mM | 0.273 ml | 1.365 ml | 2.729 ml |
5 mM | 0.055 ml | 0.273 ml | 0.546 ml |
biological activity | GW2580 is a selective CSF-1R inhibitor with an IC50 of 30 nM for c-FMS compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2, etc. are 150 to 500-fold higher selective. GW2580 (SC-203877) is a CSF-1R selective inhibitor with an IC50 of 30 nM at c-FMS, compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, the selectivity of GSK3, ITK, JAK2, etc. is 150 to 500 times higher. |
Target | Value |
c-Fms | 30 nM |