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| | 5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine Basic information |
| | 5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine Chemical Properties |
| Boiling point | 617.5±65.0 °C(Predicted) | | density | 1.252±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: soluble10mg/mL, clear (warmed) | | form | powder | | pka | 7.11±0.10(Predicted) | | color | white to beige | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| | 5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine Usage And Synthesis |
| Description | GW-2580 (870483-87-7) is a potent and selective inhibitor of cFMS receptor kinase. Completely inhibits cFMS in vitro at 60 nM with no activity against 26 other kinases1. Completely inhibits CSF-1 induced growth of mouse M-NFS-60 myeloid cells and human monocytes (at 1 μM)1. GW-2580 completely inhibits bone degradation in human osteoclasts, rat calvaria and fetal long bone1. Inhibits LPS-induced TNF production in mice. GW-2580 abrogates infiltration of macrophages into synovial joints of arthritic mice2. Active in vivo. | | Uses | GW2580 has been used to study its effect on paracrine signaling from stretched cardiomyocyte on cardiac fibroblast phenotype. | | Biochem/physiol Actions | GW2580 is a cell-permeable, potent and selective ATP-competitive inhibitor of cFMS kinase, receptor for macrophage-colony stimulating factor, M-CSF or CSF-1, and a key regulator of macrophage and osteoclast activation and differentiation. FMS is a type III receptor tyrosine kinase that binds to the macrophage or monocyte colony-stimulating factor (M-CSF or CSF-1). Overexpression of CSF-1 and/or FMS has been implicated in a number of disease states including the growth of metastasis of some types of cancer, in promoting osteoclast proliferation in bone osteolysis, and in several inflammatory disorders. GW2580 selectively inhibits cFMS-mediated cellular functions in vitro at 0.06 μM as well as CSF-1-dependent tumor growth in vivo. GW2580 was inactive against 26 other kinases. | | storage | Store at -20°C | | References | 1) Conway et al. (2005), Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580; Proc. Natl. Acad. Sci. USA, 102 16078
2) Paniagua et al. (2010), c-Fms-mediated differentiation and priming of monocyte lineage cells play a central role in autoimmune arthritis; Arthritis Res. Ther., 12 R32 |
| | 5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine Preparation Products And Raw materials |
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![5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine Structure](CAS2/GIF/870483-87-7.gif)
