Osimertinib (mesylate)
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Product Specifications
CAS Number
[1421373-66-1]
Product Name Alternative
AZD-9291 (mesylate) ; Mereletinib (mesylate)
UNSPSC
12352005
Hazard Statement
H315, H319, H335
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/AZD-9291-mesylate.html
Purity
99.97
Solubility
DMSO : 11.67 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
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
Molecular Formula
C29H37N7O5S
Molecular Weight
595.71
Precautions
H315, H319, H335
References & Citations
[1]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.|[2][2]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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
EGFR/ErbB1/HER1
Citation 01
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