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 13 Publications

5 Customer Reviews

  • Lysates from MGH121 parental cells treated with 1 μM of the indicated TKIs except for AZD9291 (160 nM) for 6 hours were probed with the indicated antibodies.

    Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560 . Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.

    Cancer Res, 2017, 77(8):2078-2089. Osimertinib (AZD9291) purchased from Selleck.

  • F, PC-9/ffluc and PC-9/LMC-GR cells (2×103 cells/well) were incubated with various concentrations of osimertinib for 72 hours. Cell viability was determined by MTT assay. Bars represent SD of quadruplicate cultures. Data shown are representative of three independent experiments with similar results.

    Mol Cancer Ther, 2017, 16(3):506-515. Osimertinib (AZD9291) purchased from Selleck.

    Western blot analysis showing phospho-EGFR (p-EGFR), total EGFR, phospho-ERK (p-ERK), total ERK, phospho-AKT (p-AKT), total AKT and β-actin as a loading control in H1975 cells treated with the indicated inhibitors. Equivalent amounts of proteins from whole cell lysates were subjected to WB analysis to detect the indicated proteins.

    J Biol Chem, 2015, 290(28): 17495-504. Osimertinib (AZD9291) purchased from Selleck.

  • J Cancer Res Clin Oncol, 2018, doi:10.1007/s00432-018-2668-7. Osimertinib (AZD9291) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

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 NInVTYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7RfZgxNTFyIN88US=> M{KzdlczKGh? NUjRUoNFcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NVG0[FBSOjV7NEi2N|M>
PC9 MX7GeY5kfGmxbjDBd5NigQ>? NGjNUI4xNTFyIN88US=> MX23NkBp NGfzN5hqdmirYnn0d{BYXCCHR1\SJIF1KGyxdzDjc45k\W62cnH0bY9vew>? NULTc2p4OjV7NEi2N|M>
PC9 GR4 M2T5UWZ2dmO2aX;uJGF{e2G7 M3\6NFAuOTBizszN NE\ucWI4OiCq MVrpcohq[mm2c9MgSWdHWiCyaH;zdIhwenmuYYTpc44h[W6mIHTve45{fHKnYX2gd4lodmGuaX7nxsA> MXKyOVk1QDZ|Mx?=
VP-2 M1jBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;GW|UxKG6P MmnDNVAh\A>? MX;EUXNQ NIfBSmNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MXiyOVQ4PzN{NR?=
PC-9/ERc1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTUWmo2OCCwTR?= NWq2UYZsOTBiZB?= NV;W[3lnTE2VTx?= NGL4N5BqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= NIr3eIUzPTR5N{OyOS=>
PC-9/BRc1 NXW5dW05T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LuVVUxKG6P Mo\NNVAh\A>? NFjWdJpFVVOR MX7pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? Mk[zNlU1Pzd|MkW=
VP-2 MknTSpVv[3Srb36gRZN{[Xl? NE\lXYw2OCCwTR?= M2m1cFI1KGh? MVfEUXNQ M3Pwe4lv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN MXqyOVQ4PzN{NR?=
PC-9/ERc1 MVLGeY5kfGmxbjDBd5NigQ>? NHrrWpA2OCCwTR?= MWiyOEBp M3PXTGROW09? NXn0T4V3cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> M2HRNVI2PDd5M{K1
PC-9/BRc1 NIrPU|NHfW6ldHnvckBCe3OjeR?= M1vYW|UxKG6P NVHTbG5JOjRiaB?= MoDvSG1UVw>? MXXpcoR2[2W|IHX4dJJme3Orb36gc4YhfGinIIDyc4Fxd3C2b4TpZ{BDS0xvMjDmZY1qdHlibXXtZoVzKEKLTR?= NXrOb2xGOjV2N{ezNlU>

... 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]

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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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01951599 Completed Healthy Volunteers AstraZeneca October 9 2013 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
NCT02157883 Active not recruiting Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer AstraZeneca November 6 2014 Phase 1
NCT02228369 Active not recruiting EGFR Mutation Positive Advanced Non Small Cell Lung Cancer AstraZeneca November 5 2014 Phase 1
NCT02143466 Recruiting Advanced Non Small Cell Lung Cancer AstraZeneca August 5 2014 Phase 1
NCT02197247 Active not recruiting Non Small Cell Lung Cancer AstraZeneca December 4 2014 Phase 1

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