Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties was written by Lee, Jung Wuk;Park, Jiwon;Kim, Jina;Kim, Jihyung;Choi, Changyu;Min, Kyung Hoon. And the article was included in European Journal of Medicinal Chemistry in 2021.HPLC of Formula: 1150566-27-0 This article mentions the following:
Tumor-associated macrophages (TAMs) are predominantly associated with tumor growth. Colony-stimulating factor 1 receptor (CSF1R) acts as a key regulator of TAM survival and differentiation and is a mol. target for cancer therapies. Herein, novel CSF1R inhibitors were identified through a replacement strategy for the hinge-binding moiety. The introduction of imidazo[1,2-a]pyridine I or pyrazolo[1,5-a]pyridine II as hinge binders led to 87% and 82% inhibition at 10 nM for CSF1R in the enzymic assay, with IC50 values of 25 nM and 27 nM in MNFS60 cells, resp. These derivatives significantly inhibited CSF1R phosphorylation in cells. Author approach could be utilized as a strategy to discover novel kinase inhibitors. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0HPLC of Formula: 1150566-27-0).
Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazine has the elements of symmetry for the point group D2h. It has three mutually perpendicular two-fold axes. It also has three mutually perpendicular planes of symmetry. As a result, pyrazine also has a centre of symmetry. Substituted pyrazines have been found as subunits of multiple synthetically constructed therapeutic agents, as well as several natural products.HPLC of Formula: 1150566-27-0