Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group was written by Zhao, Jichen;Zhang, Dehui;Zhang, Weihe;Stashko, Michael A.;DeRyckere, Deborah;Vasileiadi, Eleana;Parker, Rebecca E.;Hunter, Debra;Liu, Qingyang;Zhang, Yuewei;Norris-Drouin, Jacqueline;Li, Bing;Drewry, David H.;Kireev, Dmitri;Graham, Douglas K.;Earp, Henry Shelton;Frye, Stephen V.;Wang, Xiaodong. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 1375301-91-9 This article mentions the following:
Although all kinases share the same ATP binding pocket, subtle differences in the residues that form the pocket differentiate individual kinases’ affinity for ATP competitive inhibitors. The authors have found that by introducing a single Me group, the selectivity of the MERTK inhibitors over another target, FLT3, was increased up to 1000-fold (compound I). Compound II was identified as an in vivo tool compound with subnanomolar activity against MERTK and 38-fold selectivity over FLT3 in vitro. The potency and selectivity of II for MERTK over FLT3 were confirmed in cell-based assays using human cancer cell lines. Compound II had favorable pharmacokinetic properties in mice. Phosphorylation of MERTK was decreased by 75% in bone marrow leukemia cells from mice treated with II compared to vehicle-treated mice. In the experiment, the researchers used many compounds, for example, 2-Cyclopropyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine (cas: 1375301-91-9Recommanded Product: 1375301-91-9).
2-Cyclopropyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine (cas: 1375301-91-9) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Recommanded Product: 1375301-91-9
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia