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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 Î¼M	72 h		inhibits cell growth dose dependently	25948633
PC9	Function Assay	0-10 Î¼M	72 h		inhibits WT EGFR at low concentrations	25948633
PC9 GR4	Function Assay	0-10 Î¼M	72 h		inhibitsÂ EGFR phosphorylation and downstream signalingÂ	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]