Osimertinib Mesylate
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 Osimertinib Mesylate

CAS No.:1421373-66-1
Formula:C29H37N7O5S
Type:Pharmaceutical API
Appearance:Powder
Certificate:GMP, COPP, WC, DMF
Shelf Life:2 years
Quality Standard:CP, EP, JP, USP
Assay:98.0%-102.0%
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
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Osimertinib mesylate is a methanesulfonate (mesylate) salt prepared from equimolar amounts of osimertinib and methanesulfonic acid. It is used for treatment of EGFR T790M mutation positive non-small cell lung cancer. It has a role as an antineoplastic agent and an epidermal growth factor receptor antagonist. It contains an osimertinib(1+).

Osimertinib Mesylate is the mesylate salt form of osimertinib , a third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib  covalently binds to and inhibits the activity of numerous mutant forms of EGFR, including the secondarily-acquired resistance mutation T790M, L858R, and exon 19 deletions, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine  kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.


Function


1.EGFR Tyrosine Kinase Inhibition: Osimertinib mesylate is designed to specifically target and bind to mutated forms of the EGFR protein in cancer cells. It acts as a selective EGFR tyrosine kinase inhibitor (TKI), blocking the activity of the mutated EGFR protein.

2.Mutation-Selective Action: Osimertinib mesylate has a higher affinity for certain EGFR mutations, such as the T790M mutation, which is a common resistance mechanism to other EGFR TKIs. By inhibiting this specific mutation, Osimertinib can effectively suppress the growth and survival of cancer cells with T790M mutations.

3.Treatment of NSCLC with EGFR Mutations: Osimertinib mesylate is primarily used for the treatment of metastatic NSCLC that has specific EGFR mutations, including exon 19 deletions and exon 21 L858R mutations. It is also approved for patients with NSCLC who have developed resistance to other EGFR TKIs due to the acquisition of the T790M mutation.


Package


0.5kg/bag or 1kg/bag or according to customer’s requirements.





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