eCF309: a potent, selective and cell-permeable mTOR inhibitor was written by Fraser, Craig;Carragher, Neil O.;Unciti-Broceta, Asier. And the article was included in MedChemComm in 2016.COA of Formula: C4H7BrO2 This article mentions the following:
Kinase inhibitors capable of blocking the phosphorylation of protein substrates with high selectivity are essential to probe and elucidate the etiol. role of such mols. and their signalling pathways. By addressing these biochem. questions in disease relevant cell-based and in vivo models, strong pharmacol. evidence can be generated towards validating or disproving a target hypothesis. Pharmacol. studies can also provide fundamental information to identify appropriate biomarkers and rational drug combination strategies and thereby facilitate clin. translation. However, due to the high number of kinases encoded by the human genome (>500) and their highly conserved catalytic domains, the development of such an elite class of inhibitors-a.k.a. high-quality chem. probes-represents a major challenge. Through a ligand-based inhibitor design, focused library synthesis and phenotypic screening to prioritize compounds with potent cell activity, we recently identified a cell cycle inhibitor with micromolar potency that inhibits mTOR kinase activity. Following a rapid lead optimization campaign, we report the development of eCF309, an mTOR inhibitor displaying low nanomolar potency both in vitro and in cells and an excellent selectivity profile (S-score (35%) = 0.01 at 10 μM). In the experiment, the researchers used many compounds, for example, 2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8COA of Formula: C4H7BrO2).
2-Bromomethyl-1,3-dioxolane (cas: 4360-63-8) belongs to dioxole derivatives. Dioxoles, particularly fluorinated dioxoles, are used as co-monomers to make polymers that find use in forming protective coatings for chemical resistance. 1,3-Benzodioxole can be synthesized from catechol with disubstituted halomethanes.COA of Formula: C4H7BrO2
Referemce:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem