《Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors》 was written by Tsang, Jonathan E.; Urner, Lorenz M.; Kim, Gyudong; Chow, Kingsley; Baufeld, Lynn; Faull, Kym; Cloughesy, Timothy F.; Clark, Peter M.; Jung, Michael E.; Nathanson, David A.. HPLC of Formula: 4248-19-5 And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:
The epidermal growth factor receptor (EGFR) is genetically altered in nearly 60% of glioblastoma tumors; however, tyrosine kinase inhibitors (TKIs) against EGFR have failed to show efficacy for patients with these lethal brain tumors. This failure is attributed to the inability of clin. tested EGFR TKIs to cross the blood-brain barrier (BBB) and achieve adequate pharmacol. levels to inhibit various oncogenic forms of EGFR that drive glioblastoma. Through SAR anal., we developed compound 5 (JCN037)(I) from an anilinoquinazoline scaffold by ring fusion of the 6,7-dialkoxy groups to reduce the number of rotatable bonds and polar surface area and by introduction of an ortho-fluorine and meta-bromine on the aniline ring for improved potency and BBB penetration. Relative to the conventional EGFR TKIs erlotinib and lapatinib, JCN037 displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model. In addition to this study using tert-Butyl carbamate, there are many other studies that have used tert-Butyl carbamate(cas: 4248-19-5HPLC of Formula: 4248-19-5) was used in this study.
tert-Butyl carbamate(cas: 4248-19-5) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.HPLC of Formula: 4248-19-5
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