Home Tools

Osimertinib

Catalog No. T2490 CAS 1421373-65-0

Synonyms: AZD-9291, Mereletinib

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Osimertinib, CAS 1421373-65-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 48.00
10 mg	In stock	$ 58.00
25 mg	In stock	$ 70.00
100 mg	In stock	$ 98.00
200 mg	In stock	$ 117.00
1 g	In stock	$ 157.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

Bulk Inquiry

Select Batch

Purity: 100%

Purity: 99.83%

Purity: 99.54%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
Targets&IC50	EGFR (WT):493.8 nM, EGFR (L858R/T790M):11.44 nM, EGFR (exon 19 deletion):12.92 nM
In vitro	In the EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models, oral administration of AZD9291 (5 mg/kg) effectively inhibits AKT and ERK signaling pathways as well as EGFR phosphorylation in tumors, leading to tumor regression.
In vivo	In mutant EGFR cell lines, AZD9291 effectively inhibits cell proliferation.
Kinase Assay	ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated[1].
Cell Research	AZD-9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved[1].

Synonyms	AZD-9291, Mereletinib
Molecular Weight	499.61
Formula	C28H33N7O2
CAS No.	1421373-65-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 22 mg/mL(44 mM)

DMSO: 92 mg/mL (184.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. 2. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. 3. Wang N, et al. Osimertinib (AZD9291) increases radio‑sensitivity in EGFR T790M non‑small cell lung cancer. Oncol Rep. 2019 Jan;41(1):77-86. 4. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. 5. Nanjo S, et al. High efficacy of third generation EGFR inhibitor AZD9291 in a leptomeningeal carcinomatosis model with EGFR-mutant lung cancer cells. Oncotarget. 2016 Jan 26;7(4):3847-56.

Citations

1. Liu Y, Lai M, Li S, et al. LS‐106, a novel EGFR inhibitor targeting C797S, exhibits anti‐tumor activities both in vitro and in vivo. Cancer Science. 2021 2. Mancini M, Thomas Q D, Bourdel S, et al. Generation and Characterization of a New Preclinical Mouse Model of EGFR-Driven Lung Cancer with MET-Induced Osimertinib Resistance. Cancers. 2021, 13(14): 3441 3. Yu J, Zhang L, Peng J, et al. Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways. Biochemical pharmacology. 2022, 195: 114864. 4. Shang J, Ning S, Chen Y, et al. MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer. Acta Pharmacologica Sinica. 2021, 42(1): 120-131 5. Jin Y, Zhang Y, Huang A, et al.Overexpression of SERPINA3 suppresses tumor progression by modulating SPOP/NF‑κB in lung cancer.International Journal of Oncology.2023, 63(2): 1-16. 6. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2). 7. Lv S, Pan Q, Lu W, et al.Tenovin 3 induces apoptosis and ferroptosis in EGFR 19del non small cell lung cancer cells.Scientific Reports.2024, 14(1): 7654.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Kinase Inhibitor Library Inhibitor Library EMA Approved Drug Library

Related Products

Related compounds with same targets

20(S)-Ginsenoside Rg3 AZ7550 hydrochloride EGFR/BRAFV600E-IN-3 EGFR-IN-88 Larotinib (E)-AG 99 BGB-102 EGFR-IN-1

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

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 n 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.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Osimertinib 1421373-65-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR AZD-9291 AZD 9291 Inhibitor Ba/F3 cells H1975 PC-9 tumor xenograft model ErbB-1 AZD9291 HER1 inhibit cancer Mereletinib Epidermal growth factor receptor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.