AZD3759 1626387-80-1

Model Number: QQM25-#0562 Brand Name: QQM Key Specifications/Special Features: M weight: 459.9Storage: store the product under the recommended conditions in the certificate of analysisFormula: CHClFNOCAS no: 1626387-80-1Solvent and solubility: 10mM in DMSOAZD3759 is a potent, oral active, central nervous system-penetrant, EGFR inhibitor At Km ATP concentrations, the IC50 values were 0.3, 0.2 and 0.2nM for EGFR TK wild-type, L858R mutant, Exon 19Del enzymes, respectivelyIC50 value: 7.2 nM (L858R pEGFR)Target: EGFRIn vitro: inhibition of AZD3759 against EGFR tyrosine kinase (EGFR TK) wild type and mutant enzymes was tested at their corresponding Km and 2mM ATP concentrationsAZD3759 demonstrated inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255AZD3759 was selected as the candidate for comprehensive biological profilingin vivo: AZD3759 exhibits the best pharmacokinetic profile with moderate blood clearance at 17 mL/min/kg and volume of distribution of 5.2L/kg
Intrinsic clearance (Clint) of AZD3759 is 11.4μL/min 106 cells in human hepatocytes and the predicted clearance of the agent in humans is 7.7mL/min/kg by extrapolation (IVIVe)