Osimertinib (AZD9291)

Catalog No.S7297 Batch:S729707

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Technical Data

Formula

C28 H33 N7 O2
Molecular Weight 499.61 CAS No. 1421373-65-0
Solubility (25°C)* In vitro DMSO 99 mg/mL (198.15 mM)
Ethanol 99 mg/mL (198.15 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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]
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]
Features Orally bioavailable mutant-selective EGFR inhibitor that has been tested in Phase III clinical trials for treatment of Non-Small Cell Lung Cancer.

Protocol (from reference)

Kinase Assay:

[1]
  • EGFR cellular phosphorylation assay

    Cells are seeded (10000 cells/well) in growth medium in Corning black, clear- bottomed 384-well plates and incubated at 37°C with 5% CO2 overnight. Cells are acoustically dosed using an Echo 555, with compounds serially diluted in 100% DMSO. Plates are incubated for a further 2h, then following aspiration of medium, 40μL lx lysis buffer is added to each well. Greiner black high bind 384-well plates are coated with capture antibody and then blocked with 3% BSA. Following removal of block, 15μL of lysate are transferred to the Greiner black high bind 384-well plates and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL, of detection antibody were added and incubated for 2 hours. Following aspiration and washing of the plates with PBS, 20μL of QuantaBlu fluorogenic peroxidase substrate are added and incubated for 1 hour. 20μL QuantaBlu stop solution are added to plates and fluorescence read on an Envision plate reader using Excitation 352nm wavelength and emission 460nm wavelength. The data obtained with each compound is exported into a suitable software package to perform curve fitting analysis. From this data an IC50 value is determined by calculation of the concentration of compound that is required to give a 50% effect.
Cell Assay:

[3]
  • Cell lines

    PC9 cells

  • Concentrations

    10, 50, & 100 nM

  • Incubation Time

    24 h

  • Method

    Cells were treated with increasing concentrations of osimertinib for 24h.
Animal Study:

[2]
  • Animal Models

    Mice bearing PC9 and H1975 xenograft tumors

  • Dosages

    ~5 mg/kg

  • Administration

    p.o.

References

  • http://www.google.com/patents/WO2013014448A1?cl=en
  • http://mct.aacrjournals.org/content/12/11_Supplement/A109
  • https://pubmed.ncbi.nlm.nih.gov/35353542/

Customer Product Validation

, , Cancer Res, 2017, 77(8):2078-2089

Data from [ , , J Thorac Oncol, 2017, 12(5):884-889 ]

Data from [ , , J Thorac Oncol, 2018, 13(7):915-925 ]

Data from [ , , Clin Cancer Res, 2017, 23(12):3139-3149 ]

Selleck's Osimertinib (AZD9291) has been cited by 476 publications

Intratumor heterogeneity of EGFR expression mediates targeted therapy resistance and formation of drug tolerant microenvironment [ Nat Commun, 2025, 16(1):28] PubMed: 39747003
Itraconazole Reversing Acquired Resistance to Osimertinib in NSCLC by Inhibiting the SHH/DUSP13B/p-STAT3 Axis [ Adv Sci (Weinh), 2025, 12(7):e2409416] PubMed: 39721017
EGFR TKIs suppress MUC1 glycosylation through the PI3K/AKT/SP1/C1GALT1 pathway to enhance TnMUC1 CAR-T efficacy in EGFR-mutant NSCLC [ Cell Rep Med, 2025, S2666-3791(25)00272-1] PubMed: 40562040
The potential of lazertinib and amivantamab combination therapy as a treatment strategy for uncommon EGFR-mutated NSCLC [ Cell Rep Med, 2025, 6(2):101929] PubMed: 39874964
Longitudinal pharmacogenomic analysis of refractory lung cancer to identify therapeutic candidates for epidermal growth factor receptor-tyrosine kinase inhibitor resistance subclones [ Exp Mol Med, 2025, 10.1038/s12276-025-01493-2] PubMed: 40615564
AP1-mediated reprogramming of EGFR expression triggers resistance to BLU-667 and LOXO-292 in RET-rearranged tumors [ J Exp Clin Cancer Res, 2025, 44(1):154] PubMed: 40405293
Targeting both wild-type EGFR and its drug-resistant mutants with erlotinib-aptamer conjugates [ Eur J Med Chem, 2025, 296:117871] PubMed: 40554308
Evaluation and modification of tumor cell isolation techniques from malignant effusions for rapid drug sensitivity testing [ Mol Oncol, 2025, 10.1002/1878-0261.70072] PubMed: 40525275
Glimepiride overcomes acquired resistance to EGFR TKIs in lung cancer via the AMPK/ERK/MMP7 signaling pathway [ Biochem Pharmacol, 2025, 241:117162] PubMed: 40659128
LINC01559 drives osimertinib resistance in NSCLC through a ceRNA network regulating miR-320a/IGF2BP3 axis [ Front Pharmacol, 2025, 16:1592846] PubMed: 40313617

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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