Osimertinib (AZD9291)

Catalog No.S7297

Osimertinib (AZD9291) Chemical Structure

Molecular Weight(MW): 499.61

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.

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Cited by 35 Publications

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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 M1rkUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\RNE0yOCEQvF2= NHjMfnQ4OiCq M4D1WYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NGHXVnczPTl2OE[zNy=>
PC9 M4PRemZ2dmO2aX;uJGF{e2G7 NFGwbZYxNTFyIN88US=> NXf2VGhXPzJiaB?= NXi5R3BQcW6qaXLpeJMhX1RiRVfGVkBifCCub4egZ49v[2WwdILheIlwdnN? MYeyOVk1QDZ|Mx?=
PC9 GR4 NFzWS3NHfW6ldHnvckBCe3OjeR?= M1ruVlAuOTBizszN M3:zXFczKGh? MoXqbY5pcWKrdIRCpGVITlJicHjvd5Bpd3K7bHH0bY9vKGGwZDDkc5dve3S{ZXHtJJNq\26jbHnu[:Kh NVLRSplXOjV7NEi2N|M>
VP-2 MojVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHDVms2OCCwTR?= NHTKXpoyOCCm MkPXSG1UVw>? M4TSXIlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gcI9v\y22ZYLtJEgyOC2mYYmpJIdzd3e2aDDpcohq[mm2aX;uJIF{e2G7cx?= NG[1cnkzPTR5N{OyOS=>
PC-9/ERc1 NHrqdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonEOVAhdk1? MnX4NVAh\A>? MmDGSG1UVw>? MXHpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? MVWyOVQ4PzN{NR?=
PC-9/BRc1 NXiw[lJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLTO4M2OCCwTR?= NETST2EyOCCm MoHQSG1UVw>? MXvpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? MkjTNlU1Pzd|MkW=
VP-2 Mo[0SpVv[3Srb36gRZN{[Xl? MYK1NEBvVQ>? MoLCNlQhcA>? NFzYc3BFVVOR NUHqRoR4cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> MmHNNlU1Pzd|MkW=
PC-9/ERc1 MlGySpVv[3Srb36gRZN{[Xl? MYe1NEBvVQ>? MYqyOEBp NV\He41DTE2VTx?= MlfwbY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= MkTBNlU1Pzd|MkW=
PC-9/BRc1 NGPVbFNHfW6ldHnvckBCe3OjeR?= NFLCXIQ2OCCwTR?= NUHsSmJjOjRiaB?= NW[2Z417TE2VTx?= Mmf4bY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= M1X2eFI2PDd5M{K1

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-EGFR / p-AKT / p-ERK; 

PubMed: 28416483     


PC-9/BRc1 cells were treated with the indicated doses of osimertinib. Drugs were refreshed every 24 hours. Cellular lysates were probed with the indicated antibodies. Osim: osimertinib.

ABCB1; 

PubMed: 27649127     


The effect of osimertinib at 0.3 μM on the expression of ABCB1 was measured in KB-3-1 and KB-C2 cell lines for 0, 24, 48, and 72 h.

28416483 27649127
Growth inhibition assay
Cell viability; 

PubMed: 31043587     


Cells were treated with gefitinib or osimertinib for 72 h. Cell viability was measured by MTT assay. *P < 0.05, **P < 0.01, ***P < 0.005 by t-test.

31043587
Immunofluorescence
Ki67 / γH2AX / p16; 

PubMed: 29212784     


PC9ER cells were treated for 5 days with either 3×mAbs (20 μg/ml), saline (CTRL), or with a low dose of osimertinib (2.5 nM). Shown are representative images of cells fixed in paraformaldehyde and immunostained for KI67 (panel E), γH2AX (panel F), and p16 (panel G). DAPI counterstaining was used to follow nuclear localization. Scale bar, 20 μm. The box and whisker plots, where the ends of the box are the upper and lower quartiles, depict quantifications of results obtained in three independent experiments. **P ≤ 0.01, ***P ≤ 0.001, n = 4; one-way ANOVA with Tukey's test.

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]

Protocol

Animal Research:

[2]
+ Expand
  • Animal Models: Mice bearing PC9 and H1975 xenograft tumors
  • Formulation: --
  • Dosages: ~5 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL warmed (198.15 mM)
Ethanol 43 mg/mL warmed (86.06 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 499.61
Formula

C28 H33 N7 O2
CAS No. 1421373-65-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03257124 Recruiting Non-Small Cell Lung Cancer With EGFR T790M Mutation|With Brain and/or Leptomeningeal Metastasis|Failed Tyrosine Kinase Inhibitors Samsung Medical Center May 8 2017 Phase 2
NCT02923947 Active not recruiting Solid Tumours AstraZeneca|Quintiles Inc. May 4 2017 Phase 1
NCT03257124 Recruiting Non-Small Cell Lung Cancer With EGFR T790M Mutation|With Brain and/or Leptomeningeal Metastasis|Failed Tyrosine Kinase Inhibitors Samsung Medical Center May 8 2017 Phase 2
NCT02923947 Active not recruiting Solid Tumours AstraZeneca|Quintiles Inc. May 4 2017 Phase 1
NCT02811354 Recruiting Carcinoma Non-Small-Cell Lung National University Hospital Singapore|AstraZeneca|Singapore Clinical Research Institute February 24 2017 Phase 2
NCT02811354 Recruiting Carcinoma Non-Small-Cell Lung National University Hospital Singapore|AstraZeneca|Singapore Clinical Research Institute February 24 2017 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?

  • Answer:

    Osimertinib can be used for animal study. The vehicle we suggest is: 1% DMSO+30% PEG 300+dd H2O at up to 30mg/ml.

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EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID