Osimertinib (AZD9291)
Catalog No.S7297
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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(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.
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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.
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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.
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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.
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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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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 |
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| In vitro |
AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. [2] |
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| Cell Data |
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| 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: |
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Solubility (25°C)
| In vitro | DMSO | 99 mg/mL warmed (198.15 mM) |
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| 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
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)
*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
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 )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Can this formulation be used in mice? What are reconstitution instructions for in vivo with mice?
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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.
