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GW 2580
- Soluble in DMSO
- MF: C20H22N4O3
- MW: 366.41
Description
An orally bioavailable inhibitor of c-FMS kinase (IC50 value of 0.03 µM in vitro) and the CSF1R receptor (Kd value 1.6 nM) that competitively blocks the ATP binding site of c-FMS. GW 2580 was inactive against 26 kinases in vitro and did not inhibit the growth of mouse NS0 lymphoblastoid cells, human fibroblasts, human endothelial cells, and five human tumor cell lines. GW 2580 also interacts with TrkA, TrkB, and TrkC (Kd values 630 nM, 36 nM, and 120 nM, respectively)
More Information
| Parent CAS No. | 870483-87-7 |
|---|---|
| Chemical Name | 5-(3-methoxy-4-(4-methoxybenzyloxy)benzyl)pyrimidine-2,4-diamine |
| SMILES | C1(N)=NC=C(CC2=CC(OC)=C(OCC3=CC=C(OC)C=C3)C=C2)C(N)=N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H22N4O3/c1-25-16-6-3-13(4-7-16)12-27-17-8-5-14(10-18(17)26-2)9-15-11-23-20(22)24-19(15)21/h3-8,10-11H,9,12H2,1-2H3,(H4,21,22,23,24) |
| InChiKey | MYQAUKPBNJWPIE-UHFFFAOYSA-N |
| CID | 11617559 |
| Short Description | dual cFMS kinase/CSF1R inhibitor |
References
- JG Conway 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.
- JG Conway 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.
- MW Karaman et al. A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
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