COA of Formula: C6H11BrO2In 2019 ,《Formulation optimization of an ephrin A2 targeted immunoliposome encapsulating reversibly modified taxane prodrugs》 was published in Journal of Controlled Release. The article was written by Huang, Zhaohua Richard; Tipparaju, Suresh Kumar; Kirpotin, Dmitri B.; Pien, Christine; Kornaga, Tad; Noble, Charles O.; Koshkaryev, Alexander; Tran, Jimmy; Kamoun, Walid S.; Drummond, Daryl C.. The article contains the following contents:
Ephrin A2 targeted immunoliposomes incorporating pH-sensitive taxane prodrugs were developed for sustained delivery of active drug to solid tumors. Here we describe the systematic formulation development and characterization of these immunoliposomes. We synthesized both paclitaxel and docetaxel prodrugs to formulate as ephrin A2-targeted liposomes stabilized in the aqueous core with sucroseoctasulfate (SOS). The optimized lipid formulation was comprised of egg-sphingomyelin, cholesterol, and polyethylene glycol distearoyl glycerol (PEG-DSG). The formulations examined had a high efficiency of prodrug encapsulation (as high as 114 mol% taxane per mol phospholipid) and subsequent stability (>3 years at 2-8°C). The taxane prodrug was stabilized with extraliposomal citric acid and subsequently loaded into liposomes containing a gradient of SOS, resulting in highly stable SOS-drug complexes being formed inside the liposome. The internal prodrug and SOS concentrations were optimized for their impact on in vivo drug release and drug degradation Cryo-electron microscope images revealed dense prodrug-SOS complex in the aqueous core of the immunoliposomes. Ephrin A2-targeted taxane liposomes exhibited sub-nanomolar (0.69 nM) apparent equilibrium dissociation constant toward the extracellular domain of the ephrin A2 receptor, long circulation half-life (8-12 h) in mouse plasma, a release rate dependent on intraliposomal drug concentration and stable long-term storage. At an equitoxic dose of 50 mg taxane/kg, ephrin A2-targeted liposomal prodrug showed greater antitumor activity than 10 mg/kg of docetaxel in A549 non-small cell lung, as well as MDA-MB-436 and SUM149 triple neg. breast cancer xenograft models. The lead mol. entered a Phase I clin. trial in patients with solid tumors (NCT03076372). In the experimental materials used by the author, we found Ethyl 4-bromobutyrate(cas: 2969-81-5COA of Formula: C6H11BrO2)
Ethyl 4-bromobutyrate(cas: 2969-81-5) 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.COA of Formula: C6H11BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary