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Home > Products >  Osimertinib (AZD9291)

Osimertinib (AZD9291) CAS NO.1421373-65-0

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Keywords

  • Osimertinib
  • AZD9291
  • 1421373-65-0

Quick Details

  • ProName: Osimertinib (AZD9291)
  • CasNo: 1421373-65-0
  • Molecular Formula: C28H33N7O2
  • ProductionCapacity: Metric Ton/Day
  • Purity: >97%
  • LimitNum: 0 Metric Ton

Superiority

Biological Activity

Description Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
Features Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.
Targets
L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
WT EGFR [1]
(LoVo cells)
11.44 nM 12.92 nM 493.8 nM
In vitro

AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. [2]

Cell Data
 
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC-9/BRc1 Function Assay 50 nM 24 h DMSO induces expression of the proapoptotic BCL-2 family member BIM 25477325
PC-9/ERc1 Function Assay 50 nM 24 h DMSO induces expression of the proapoptotic BCL-2 family member BIM 25477325
VP-2 Function Assay 50 nM 24 h DMSO induces expression of the proapoptotic BCL-2 family member BIM 25477325

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot   28416483 27649127
Growth inhibition assay 31043587
Immunofluorescence 29212784
In vivo AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. [2]

 

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