GW2580-d6

GW2580-d6 is the deuterium labeled GW2580. GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling[1].

Product Specifications

CAS Number

[2733770-48-2]

UNSPSC

12352005

Target

C-Fms; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Field of Research

Inflammation/Immunology; Cancer

Purity

98.36

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

NC1=NC(N)=C(CC2=CC(OC([2H])([2H])[2H])=C(OCC3=CC=C(OC([2H])([2H])[2H])C=C3)C=C2)C=N1

Molecular Formula

C20H16D6N4O3

Molecular Weight

372.45

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Conway JG, et al. 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.|[3]Priceman SJ, et al. Targeting distinct tumor-infiltrating myeloid cells by inhibiting CSF-1 receptor: combating tumor evasion of antiangiogenic therapy. Blood. 2010 Feb 18;115 (7) :1461-71|[4]Conway JG, 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. 2008 Jul;326 (1) :41-50.