AZD-9291 mesylate; Mereletinib mesylate MedChemExpress (MCE)

Product Name	Osimertinib Mesylate
Synonyms	Osimertinib AZD-9291 (Mesylate) Osimertinib Mesylate Osimertinib mesylate Mereletinib mesylate Osimertinib Mesylate(AZD9291) N-[2-(2-dimethylaminoethylmethylamino)-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide mesylate salt
CAS	1421373-66-1
EINECS	200-064-1
Chemical Formula	C28H33N7O2.CH4O3S
Molecular Weight	595.71298
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Package	10 mM * 1 mL;1 mg;5 mg;10 mg;50 mg;100 mg;200 mg;500 mg
Price	Email to quote
Descriptions	Osimertinib mesylate Osimertinib mesylate MedChemExpress (MCE) HY-15772A 1421373-66-1 AZD-9291 mesylate Descriptions Osimertinib mesylate Osimertinib mesylate MedChemExpress (MCE) HY-15772A 1421373-66-1 AZD-9291 mesylate Mereletinib mesylate 99.97% 4°C, sealed storage, away from moisture In solvent : -80°C, 2 years -20°C, 1 year (sealed storage, away from moisture) Room temperature in continental US may vary elsewhere. 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. Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for Osimertinib. Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM[1]. The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays 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]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day[2]. EGFRL858R/T790M 1 nM (IC50) EGFRL858R 12 nM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]* [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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