G-5903 GW2580, Free Base, >99%

Related Terms : [cFMS Receptor Tyrosine Kinase Inhibitor] [CSF-1 Receptor Inhibitor]

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  • 100 mg
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  • 300 mg
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  • 1 g
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  • 5 g
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  • 10 g
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  • M.W. 366.41
  • C20H22N4O3
  • [870483-87-7]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 40 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 20-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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  • GW2580 is a small-molecule inhibitor of cFMS kinase; at 60 nM it inhibited human cFMS kinase completely in vitro and was inactive against 26 other kinases. GW2580 inhibited lipopolysaccharide (LPS)-induced TNF production in mice, but not LPS-induced TNF production in freshly isolated human monocytes and mouse macrophages in vitro. Also, GW2580 at 1 µM totally inhibited CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes, and prevented bone degradation in cultures of rat calvaria and rat fetal long bone in vitro. Conway, J.G., et al. "Inhibition of colony-stimulating-factor-1 signaling in vitro with the orally bioavailable cFMS kinase inhibitor GW2580." Proc. Natl. Acad. Sci. USA 102: 16078-16083 (2005).
  • In an arthritic rat model, GW2580 inhibited joint connective tissue and bone destruction, and thus preserved joint integrity. Conway, J.G., et al. "Effects of the cFMS kinase inhibitor 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine (GW2580) in normal and arthritic rats." J. Pharmacol. Exp. Ther. 326: 41-50 (2008).
  • Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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