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Osimertinib dimesylate Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752751

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

Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Osimertinib dimesylate, Inhibitor
Full Product Name
Osimertinib dimesylate
Product Synonym Names
AZD-9291 (dimesylate); Mereletinib (dimesylate)
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
691.82
Solubility
DMSO: 0.4mg/mL (0.58mM) Need ultrasonic and warming
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C30H41N7O8S2
SMILES
CS(=O)(O)=O.C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.CS(=O)(O)=O
CAS Number
2070014-82-1
Target & IC50
EGFRL858R: ic50 12nM
EGFRL858R/T790M: ic50 1nM
In Vitro
The tumor-bearing mice are treated with Osimertinib (5mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice display nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib, while 5 of 5 mice treated with vehicle shows tumor growth [1]. Upon dosing Osimertinib in three efficacy models, comparable efficacy is observed at relatively low doses (10mg/kg per day). The excellent efficacy is also observed when Osimertinib is dosed at 5mg/kg per day [2].

Product References and Citations for Osimertinib dimesylate, inhibitor

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.
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.
Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.
Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

Other Notes

Small volumes of Osimertinib dimesylate, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Osimertinib dimesylate purchase

MBS5752751 is an inhibitor targeting Osimertinib dimesylate.
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