Yao, Yuqin published the artcileDesign, synthesis and pharmacological evaluation of 4-(3-chloro-4-(3-cyclopropylthioureido)-2-fluorophenoxy)-7-methoxyquinoline-6-carboxamide (WXFL-152): a novel triple angiokinase inhibitor for cancer therapy, Recommanded Product: 1,1,1-Trifluoropropan-2-amine, the publication is Acta Pharmaceutica Sinica B (2020), 10(8), 1453-1475, database is CAplus and MEDLINE.
In this study, the design, synthesis, target identification, mol. mechanism, pharmacodynamics (PD) and pharmacokinetics (PK) research of a novel triple-angiokinase inhibitor WXFL-152 is reported. WXFL-152, identified from a series of 4-oxyquinoline derivatives based on a structure-activity relationship study, inhibited the proliferation of vascular endothelial cells (ECs) and pericytes by blocking the angiokinase signals VEGF/VEGFR2, FGF/FGFRs and PDGF/PDGFRb simultaneously in vitro. Significant anticancer effects of WXFL-152 were confirmed in multiple preclin. tumor xenograft models, including a patient-derived tumor xenograft (PDX) model. Pharmacokinetic studies of WXFL-152 demonstrated high favorable bioavailability with single-dose and continuous multi-dose by oral administration in rats and beagles. In conclusion, WXFL-152, which is currently in phase Ib clin. trials, is a novel and effective triple-angiokinase inhibitor with clear PD and PK in tumor therapy.
Acta Pharmaceutica Sinica B published new progress about 421-49-8. 421-49-8 belongs to catalysis-chemistry, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain, name is 1,1,1-Trifluoropropan-2-amine, and the molecular formula is C18H17N5O3, Recommanded Product: 1,1,1-Trifluoropropan-2-amine.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia