OSIMERTINIB MESYLATE

Alias: AZD-9291 mesylate; Mereletinib mesylate; AZD9291; AZD 9291; Trade name: Tagrisso

Cat No.:V3975 Purity: ≥98%

COA Product Data Instructions for use SDS

OSIMERTINIB MESYLATE Chemical Structure CAS No.: 1421373-66-1
Product category: EGFR

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of OSIMERTINIB MESYLATE:

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Osimertinib mesylate (formerly known as AZD9291; AZD-9291; AZD 9291; mereletinib; Tagrisso), the mesylate salt of osimertinib, is a novel, potent, oral bioavailable, irreversible, and mutant-selective, 3rd generation EGFR inhibitor approved by both FDA and the European Commission for cancer treatment. In LoVo cells, it inhibits WT EGFR, L858R/T790M EGFR, and Exon 19 deletion EGFR with IC50 values of 12.92, 11.44, and 493.8 nM, respectively.

Biological Activity I Assay Protocols (From Reference)

Targets

EGFR^L858R/T790M (IC50 = 1 nM); EGFR^L858R (IC50 = 12 nM)

ln Vitro

METTL7B is expressed at a higher level in lung adenocarcinoma (LUAD) cells that are resistant to osimertinib than in cells that are sensitive to the drug. LUAD cells were re-sensitized to osimertinib after METTL7B was knocked down using GNC-siRNA.[1]

ln Vivo

METTL7B is considerably higher in osimertinib-resistant xenografts than in osimertinib-sensitive xenografts at the mRNA and protein levels. Combining GNC-siMETTL7B (6 mg siRNA per mouse equivalent) with osimertinib (30 mg/kg) treatment significantly suppresses tumor growth in the LUAD CDX mouse model.

Enzyme Assay

Osimertinib, formerly known as mereletinib and AZD-9291, is a third generation EGFR inhibitor that is available orally and is irreversible. It selectively targets specific mutants of EGFR, with IC50 values of 493.8 nM for wild-type EGFR in LoVo cells, L858R/T790M EGFR, and Exon 19 deletion EGFR, respectively. It reduces the side effects associated with currently available medications by inhibiting both activating and resistant EGFR mutations while protecting the normal form of EGFR found in normal skin and gut cells.

Cell Assay

In 96-well plates, cells are plated at a density of 3,000 cells per well. Addition of osimertinib to the medium results in a 72-hour treatment. Cell Counting Kit-8 is used to perform assays for cell viability.

Animal Protocol

5 mg/kg; p.o

EGFRm+ and EGFRm+/T790M transgenic mice

References

[1]. Mol Cancer . 2022 Feb 10;21(1):43.

[2]. Br J Cancer . 2019 Oct;121(9):725-737.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C29H37N7O5S
Molecular Weight	595.72
Exact Mass	595.25768848
Elemental Analysis	C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38
CAS #	1421373-66-1
Related CAS #	Osimertinib;1421373-65-0;Osimertinib-d6;1638281-44-3;Osimertinib dimesylate;2070014-82-1
Appearance	Light yellow solid powder
SMILES	CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC.CS(=O)(=O)O
InChi Key	FUKSNUHSJBTCFJ-UHFFFAOYSA-N
InChi Code	InChI=1S/C28H33N7O2.CH4O3S/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24;1-5(2,3)4/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32);1H3,(H,2,3,4)
Chemical Name	N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide;methanesulfonic acid
Synonyms	AZD-9291 mesylate; Mereletinib mesylate; AZD9291; AZD 9291; Trade name: Tagrisso
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: > 100mg/mL

Water: N/A

Ethanol: N/A

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 1% DMSO+30% PEG 300+dd H2O: 30mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.6786 mL	8.3932 mL	16.7864 mL
	5 mM	0.3357 mL	1.6786 mL	3.3573 mL
	10 mM	0.1679 mL	0.8393 mL	1.6786 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

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

Molecular mass (or 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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

Calculate Reset

Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05880706	Recruiting	Drug: Osimertinib Mesylate Tablets Drug: BL-B01D1	Non-small Cell Lung Cancer	Sichuan Baili Pharmaceutical Co., Ltd.	July 19, 2023	Phase 2
NCT05020769	Recruiting	Drug: SI-B001 Drug: Osimertinib	Non-small Cell Lung Cancer	Sichuan Baili Pharmaceutical Co., Ltd.	January 6, 2022	Phase 2 Phase 3
NCT05085054	Not yet recruiting	Drug: Osimertinib Mesylate	Non Small Cell Lung Cancer	Wuhan Union Hospital, China	June 1, 2022	Phase 2
NCT05816252	Recruiting	Drug: Osimertinib Drug: Carboplatin	Non-small Cell Lung Cancer	Klus Pharma Inc.	April 19, 2023	Phase 2
NCT05085054	Not yet recruiting	Drug: Osimertinib Mesylate	Non Small Cell Lung Cancer	Wuhan Union Hospital, China	June 1, 2022	Phase 2

Biological Data

AZD9291 binding mode and structure.Cancer Discov.2014 Sep;4(9):1046-61.
Effect of AZD9291 on EGFR phosphorylationin vitro.Cancer Discov.2014 Sep;4(9):1046-61.
In vivoanti-tumor efficacy of AZD9291 in subcutaneous xenograft models of EGFR-TKI sensitising and T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61.
AZD9291 induces significant and sustained tumor regression in transgenic models of EGFR-TKI sensitising (C/L858R) and T790M resistant (C/L+T) lung cancer.Cancer Discov.2014 Sep;4(9):1046-61.
AZD9291 inhibits EGFR phosphorylation and downstream signallng in murine models of EGFR T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61.
Proof of concept clinical studies validating AZD9291 as a mutant-selective EGFR kinase T790M inhibitor.Cancer Discov.2014 Sep;4(9):1046-61.