Development of subnanomolar radiofluorinated (2-pyrrolidin-1-yl)imidazo[1,2-b]pyridazine pan-Trk inhibitors as candidate PET imaging probes was written by Bernard-Gauthier, Vadim;Bailey, Justin J.;Aliaga, Arturo;Kostikov, Alexey;Rosa-Neto, Pedro;Wuest, Melinda;Brodeur, Garrett M.;Bedell, Barry J.;Wuest, Frank;Schirrmacher, Ralf. And the article was included in MedChemComm in 2015.Recommanded Product: 1150566-27-0 This article mentions the following:
Dysregulation of tropomyosin receptor kinases (TrkA/B/C) expression and signalling is recognized as a hallmark of numerous neurodegenerative diseases including Parkinson’s, Huntington’s and Alzheimer’s disease. TrkA/B/C is known to drive tumorogensis and metastatic potential in a wide range of neurogenic and non-neurogenic human cancers. The development of suitable positron emission tomog. (PET) radioligands would allow an in vivo exploration of this versatile potential therapeutic target. Herein, the rational remodeling of the amide moiety of a 6-(2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazine-3-amide lead structure to accommodate efficient fluorine-18 labeling led to the identification of a series of fluorinated Trk inhibitors with picomolar IC50. The ensuing representative radiolabeled inhibitors [18F]16 ([18F]-(±)-IPMICF6) and [18F]27 ([18F]-(±)-IPMICF10) constitute novel lead radioligands with about 2- to 3- orders of magnitude increased TrkB/C potencies compared to previous lead tracers and display favorable selectivity profiles and physicochem. parameters for translation into in vivo PET imaging agents. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0Recommanded Product: 1150566-27-0).
Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Recommanded Product: 1150566-27-0