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AZD9291

(CAS No:1421373-65-0)
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.
CAS No:1421373-65-0
Molecular Weight(MW):499.61
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1421373-65-0
Molecular formula(MF) C28H33N7O2
Molecular Weight(MW): 499.61
Alias
Solubility
In vitro DMSO 99 mg/mL warmed (198.15 mM)
Ethanol 43 mg/mL warmed (86.06 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% PEG 300+dd H2O 30
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
PC9 GR4 Growth Inhibition Assay 0-10 μM 72 h inhibits cell growth dose dependently 25948633
PC9 Function Assay 0-10 μM 72 h inhibits WT EGFR at low concentrations 25948633
PC9 GR4 Function Assay 0-10 μM 72 h inhibits EGFR phosphorylation and downstream signaling  25948633
VP-2 Growth Inhibition Assay 50 nM 10 d DMSO inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
PC-9/ERc1 Growth Inhibition Assay 50 nM 10 d DMSO inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
PC-9/BRc1 Growth Inhibition Assay 50 nM 10 d DMSO inhibits proliferation in long-term (10-day) growth inhibition assays 25477325
VP-2 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
PC-9/BRc1 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

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]