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Osimertinib dimesylate

Name: Osimertinib dimesylate
Brand: TargetMol
SKU: T10433
Rating: 4.5 (1 reviews)

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Catalog No. T10433Cas No. 2070014-82-1

Alias Mereletinib (dimesylate), AZD-9291 (dimesylate)

Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).

Osimertinib dimesylate

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Catalog No. T10433Alias Mereletinib (dimesylate), AZD-9291 (dimesylate)Cas No. 2070014-82-1

Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	5 days	5 days
5 mg	$39	5 days	5 days
10 mg	$55	5 days	5 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Appearance:solid

Color:White

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Product Introduction

Bioactivity

Description	Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M).
Targets&IC50	EGFR (L858R):12 nM, EGFR (L858R/T790M):1 nM
In vitro	Osimertinib (AZD-9291) exhibits similar potency to early-generation tyrosine kinase inhibitors in inhibiting EGFR phosphorylation in EGFR cells with sensitizing EGFR mutations, including PC-9 (ex19del), H3255 (L858R), and H1650 (ex19del) (mean IC50s: 13-54 nM). Additionally, Osimertinib potently inhibits EGFR phosphorylation in T790M mutant cell lines H1975 (L858R/T790M) and PC-9VanR (ex19del/T790M), with mean IC50s below 15 nM [1].
In vivo	Tumor-bearing mice are treated with Osimertinib (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 out of 5 C/L858R mice exhibit nearly 80% reduction in tumor volume by MRI, while 5 out of 5 vehicle-treated mice show tumor growth [1]. Comparable efficacy is observed at low doses (10 mg/kg per day) in three efficacy models, and excellent efficacy is also noted at 5 mg/kg per day [2].
Synonyms	Mereletinib (dimesylate), AZD-9291 (dimesylate)

Chemical Properties

Molecular Weight	691.82
Formula	C₃₀H₄₁N₇O₈S₂
Cas No.	2070014-82-1
Smiles	CS(O)(=O)=O.CS(O)(=O)=O.COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12
Relative Density.	no data available

Storage & Solubility Information

Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Solubility Information	DMSO: 0.4 mg/mL (0.58 mM), Sonication and heating are recommended.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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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