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 14 Publications

9 Customer Reviews

  • (C,D) The Ba/F3 cells expressing EGFR-T854A/C797S/del19 (C) and EGFR-T854A/C797S/L858R (D) were treated with gefitinib, afatinib, osimertinib, and brigatinib for 6 hours at indicated concentrations. EGFR phosphorylation and downstream signal pathway were evaluated by Western blotting.

    J Thorac Oncol, 2018, 13(7):915-925. Osimertinib (AZD9291) purchased from Selleck.

    (C) Immunoblotting of lysates from EGFR L858R and EGFR L858M/L861Q NIH-3T3 cells treated with the indicated concentrations of gefitinib, osimertinib, or afatinib. The ratio of phospho-EGFR in treated vs. untreated samples was quantified by densitometry for each cell line.

    J Thorac Oncol, 2017, 12(5):884-889. Osimertinib (AZD9291) purchased from Selleck.

  • Protein expression detected by Western blotting in PC-9 cells (left), PC-3 cells (middle), and PC-9BIMi2−/− cells (right), incubated with gefitinib (1 μmol/L), afatinib (1 μmol/L), or osimertinib (1 μmol/L), for 24 hours.

    Clin Cancer Res, 2017, 23(12):3139-3149. Osimertinib (AZD9291) purchased from Selleck.

    Apoptosis susceptibility of H1975 and H1975-OR NSCLC cell lines following treatment with NGI-1 (10μM), Osimertinib (1μM) or a combination of both for 48 h measured with Annexin- V and 7-AAD flow cytometry as in Fig. 1. The data represents the mean ± s.d., n = 3. *P < 0.01.

    Cancer Res, 2018, doi:10.1158/0008-5472.CAN-18-0505. Osimertinib (AZD9291) purchased from Selleck.

  • 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.
L858R/T790M EGFR [1]
(LoVo cells)
Exon 19 deletion EGFR [1]
(LoVo cells)
(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 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H1TFAuOTBizszN MnGwO|IhcA>? M4nCXolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWG3Z5M2OjV7NEi2N|M>
PC9 MVPGeY5kfGmxbjDBd5NigQ>? MXOwMVExKM7:TR?= M4\L[VczKGh? NXfUOGY{cW6qaXLpeJMhX1RiRVfGVkBifCCub4egZ49v[2WwdILheIlwdnN? M4rwSlI2QTR6NkOz
PC9 GR4 M37tR2Z2dmO2aX;uJGF{e2G7 MXywMVExKM7:TR?= NFiyPXg4OiCq NFnFNmRqdmirYnn0d:KhTUeIUjDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0he2mpbnHsbY5oyqB? NHrGNGkzPTl2OE[zNy=>
VP-2 NELESIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYK1NEBvVQ>? M1\MOFExKGR? NYm0NYExTE2VTx?= MnLmbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDsc45oNXSncn2gLFExNWSjeTmg[5Jwf3SqIHnubIljcXSrb36gZZN{[Xm| Mn\JNlU1Pzd|MkW=
PC-9/ERc1 NGL0SWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV21NEBvVQ>? Mli5NVAh\A>? MXzEUXNQ NVnrfXE2cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBtd26pLYTldo0hMDFyLXThfUkh\3Kxd4ToJIlvcGmkaYTpc44h[XO|YYnz NYHtPFNxOjV2N{ezNlU>
PC-9/BRc1 NGPn[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnCblg2OCCwTR?= MkHVNVAh\A>? NETXR3BFVVOR NGnNR5dqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIxwdmdvdHXycUApOTBvZHH5LUBoem:5dHigbY5pcWKrdHnvckBie3OjeYO= MX[yOVQ4PzN{NR?=
VP-2 MluySpVv[3Srb36gRZN{[Xl? MVi1NEBvVQ>? MkPvNlQhcA>? M{HCfmROW09? NXvmenF5cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NIXLe2kzPTR5N{OyOS=>
PC-9/ERc1 NUn1Z21oTnWwY4Tpc44hSXO|YYm= MkHrOVAhdk1? M17sXFI1KGh? MXzEUXNQ M2\JVolv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN Ml;pNlU1Pzd|MkW=
PC-9/BRc1 MmXtSpVv[3Srb36gRZN{[Xl? M2HBWlUxKG6P MkHTNlQhcA>? M4nQZWROW09? M{X4Uolv\HWlZYOg[ZhxemW|c3nvckBw\iC2aHWgdJJw[XCxcITveIlkKEKFTD2yJIZidWmueTDt[Y1j\XJiQlnN NG\2fZIzPTR5N{OyOS=>

... 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]


Animal Research:


+ 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.

* 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

C28 H33 N7 O2

CAS No. 1421373-65-0
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Molarity Calculator

Mass Concentration Volume Molecular Weight

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 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
NCT02972333 Not yet recruiting EGFR-TKI Resistant Mutation|Nonsmall Cell Lung Cancer|AZD9291|Brain Metastases Shandong Cancer Hospital and Institute|AstraZeneca December 2016 Phase 3
NCT02997501 Active not recruiting Lung Cancer AstraZeneca|TigerMed December 23 2016 Phase 3
NCT02771314 Recruiting Non Small Cell Lung Cancer Hellenic Oncology Research Group June 2016 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

If you have any other enquiries, please leave a message.

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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.

EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID