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 16 Publications

9 Customer Reviews

  • 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.

  • (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.

  • 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 NHnISnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm1NE0yOCEQvF2= NHzveo44OiCq M4DOZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NYjtUWhnOjV7NEi2N|M>
PC9 MkLaSpVv[3Srb36gRZN{[Xl? Mlz3NE0yOCEQvF2= NWm4NZVxPzJiaB?= M{\rSolvcGmkaYTzJHdVKEWJRmKgZZQhdG:5IHPvcoNmdnS{YYTpc45{ MlLBNlU6PDh4M{O=
PC9 GR4 NWntOGFQTnWwY4Tpc44hSXO|YYm= MoPTNE0yOCEQvF2= M4C4OVczKGh? NEfEUlBqdmirYnn0d:KhTUeIUjDwbI9{eGixconsZZRqd25iYX7kJIRwf26|dILlZY0he2mpbnHsbY5oyqB? NIXlXJozPTl2OE[zNy=>
VP-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK2XXFPPTBibl2= MknpNVAh\A>? MnL4SG1UVw>? MYnpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? NV3xXGI5OjV2N{ezNlU>
PC-9/ERc1 NH[4TJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUG1NEBvVQ>? NF3uXIcyOCCm NUP3U5E2TE2VTx?= Mk\LbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDsc45oNXSncn2gLFExNWSjeTmg[5Jwf3SqIHnubIljcXSrb36gZZN{[Xm| M3\IZ|I2PDd5M{K1
PC-9/BRc1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLPOVAhdk1? NF7zR4MyOCCm MV3EUXNQ MWDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHzvcocufGW{bTCoNVAu\GG7KTDndo94fGhiaX7obYJqfGmxbjDhd5NigXN? M3HreVI2PDd5M{K1
VP-2 M4fsOmZ2dmO2aX;uJGF{e2G7 M1;MSFUxKG6P MV[yOEBp MUjEUXNQ NWDkS2R[cW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NUDGbJF{OjV2N{ezNlU>
PC-9/ERc1 M2SzeWZ2dmO2aX;uJGF{e2G7 NUPybYtmPTBibl2= M2rCPFI1KGh? MX\EUXNQ NWnpO4JScW6mdXPld{BmgHC{ZYPzbY9vKG:oIITo[UBxem:jcH;weI91cWNiQlPMMVIh\mGvaXz5JI1mdWKncjDCTW0> NX\XOGJoOjV2N{ezNlU>
PC-9/BRc1 Mmr3SpVv[3Srb36gRZN{[Xl? NHHvNJk2OCCwTR?= NUOyb2wxOjRiaB?= M2HkSmROW09? MnfObY5lfWOnczDlfJBz\XO|aX;uJI9nKHSqZTDwdo9ieG:ydH;0bYMhSkOOLUKg[oFucWy7IH3lcYJmeiCESV2= NGrrVVkzPTR5N{OyOS=>

... 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

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

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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 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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID