《Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3》 was written by Li, Zhihong; Wang, Xianghong; Eksterowicz, John; Gribble, Michael W.; Alba, Grace Q.; Ayres, Merrill; Carlson, Timothy J.; Chen, Ada; Chen, Xiaoqi; Cho, Robert; Connors, Richard V.; DeGraffenreid, Michael; Deignan, Jeffrey T.; Duquette, Jason; Fan, Pingchen; Fisher, Benjamin; Fu, Jiasheng; Huard, Justin N.; Kaizerman, Jacob; Keegan, Kathleen S.; Li, Cong; Li, Kexue; Li, Yunxiao; Liang, Lingming; Liu, Wen; Lively, Sarah E.; Lo, Mei-Chu; Ma, Ji; McMinn, Dustin L.; Mihalic, Jeffrey T.; Modi, Kriti; Ngo, Rachel; Pattabiraman, Kanaka; Piper, Derek E.; Queva, Christophe; Ragains, Mark L.; Suchomel, Julia; Thibault, Steve; Walker, Nigel; Wang, Xiaodong; Wang, Zhulun; Wanska, Malgorzata; Wehn, Paul M.; Weidner, Margaret F.; Zhang, Alex J.; Zhao, Xiaoning; Kamb, Alexander; Wickramasinghe, Dineli; Dai, Kang; McGee, Lawrence R.; Medina, Julio C.. Recommanded Product: 3-Bromo-2-fluoro-4-iodopyridine And the article was included in Journal of Medicinal Chemistry on April 24 ,2014. The article conveys some information:
The authors describe the structural optimization of a lead compound that exhibits dual inhibitory activities against FLT3 and CDK4. A series of pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyrimidine derivatives was synthesized, and SAR anal., using cell-based assays, led to the discovery of AMG 925 (I), a potent and orally bioavailable dual inhibitor of CDK4 and FLT3, including many FLT3 mutants reported to date. Compound I inhibits the proliferation of a panel of human tumor cell lines including Colo205 (Rb+) and U937 (FLT3WT) and induced cell death in MOLM13 (FLT3ITD) and even in MOLM13 (FLT3ITD, D835Y), which exhibits resistance to a number of FLT3 inhibitors currently under clin. development. At well-tolerated doses, compound I leads to significant growth inhibition of MOLM13 xenografts in nude mice, and the activity correlates with inhibition of STAT5 and Rb phosphorylation.3-Bromo-2-fluoro-4-iodopyridine(cas: 884494-52-4Recommanded Product: 3-Bromo-2-fluoro-4-iodopyridine) was used in this study.
3-Bromo-2-fluoro-4-iodopyridine(cas: 884494-52-4) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Recommanded Product: 3-Bromo-2-fluoro-4-iodopyridine
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com