AZD-9291 mesylate (Osimertinib,Mereletinib),1421373-66-1

公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!

YZ剂描述：

产品名称：AZD-9291 mesylate (Osimertinib,Mereletinib)

产品别名：Mereletinib mesylate; EGFR inhibitor; AZD9291 mesylate; AZD 9291 mesylate，Tagrisso

英文别名：Mereletinib mesylate;EGFR inhibitor;AZD9291 mesylate;AZD 9291 mesylate;Tagrisso

靶点：EGFR

CAS：1421373-66-1

纯度：>99%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).

溶解性：DMSO

体外研究：

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.

体内研究：The tumor-bearing mice are treated with 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 AZD-9291, while 5 of 5 mice treated with vehicle shows tumor growth. 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. AZD-9291 also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing 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 AZD-9291 is dosed at 5 mg/kg per day.

产品信息订购：

产品更多信息请进入爱必信网站咨询