In 2022,Bhumireddy, Archana; Bandaru, N. V. M. Rao; Raghurami Reddy, B.; Gore, Suraj T.; Mukherjee, Subhendu; Balasubramanian, Wesley Roy; Sumanth Kumar, V.; Alapati, Krishna Satya; Venkata Gowri Chandra Sekhar, Kondapalli; Nellore, Kavitha; Abbineni, Chandrasekhar; Samajdar, Susanta published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders》.Recommanded Product: Ethyl 5-bromovalerate The author mentioned the following in the article:
Multiple Splice variants of AR have been reported in the past few years. These splice variants are upregulated in most cases of CRPC resulting in poor prognosis. Most of these variants lack the ligand binding domain (LBD) but still bind to DNA resulting in constitutive activation of downstream targets. The AR-V7 splice variant has been characterized extensively and current clin. trials in CRPC are exploring the use of AR-V7 as a biomarker. New therapeutic mols. that selectively target AR-V7 are also being explored. However, there is a dearth of information available on the selectivity, phenotypic responses in AR-V7 dependent cell lines and pharmacokinetic properties of such mols. Using our proprietary computational algorithms and rational SAR optimization, we have developed a potent and selective AR-V7 degrader from a known AR DNA binding domain (DBD) binder. This mol. effectively degraded AR-V7 in a CRPC cell line and demonstrated good oral bioavailability in mouse PK studies. This tool compound can be used to evaluate the pharmacol. effects of AR-V7 degraders. Further exploration of SAR can be pursued to develop more optimized lead compoundsEthyl 5-bromovalerate(cas: 14660-52-7Recommanded Product: Ethyl 5-bromovalerate) was used in this study.
Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Recommanded Product: Ethyl 5-bromovalerate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary