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CAS No.: N/A

AZD9291 Dimesylate Catalog No. CSN19270

Synonyms: AZD9291 Dimesylate; Mereletinib Dimesylate

Osimertinib Dimesylate 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).

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技术信息

生物活性

描述EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1–4) with an external domain that binds activating ligands, such as EGF. EGFR T790M mutation is the most common mechanism of drug resistance. Osimertinib is an irreversible EGFR inhibitor which more potent to mutant-selective EGFR with IC₅₀ values of 12.92 nM, 11.44 nM and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR and WT EGFR, with a 200-fold selectivity for T790M/L858R over wild type EGFR, in LoVo cells, respectively^[1]. Osimertinib potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; <25 nM) and EGFRm+/T790M (e.g. H1975; <25 nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo; >500 nM). Consistent with that, Osimertinib showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. Oral administration of Osimertinib once daily at dose of 5 mg/kg caused profound regression of tumors across EGFRm+ (PC9; 178% growth inhibition) and EGFRm+/T790M (H1975; 119% growth inhibition) tumor models in vivo, after 14 days dosing, and this was associated with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK. Chronic long-term treatment of PC9 and H1975 xenograft tumors with Osimertinib led to a complete and sustained macroscopic response, with no visible tumors after 40 days dosing, and being maintained beyond 100 days^[2].
作用机制Osimertinib may bind to T790M EGFR kinase in the ATP-binding domain (such as T790M and C797S).^[3]

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4455 mL
- 7.2273 mL
- 14.4546 mL
- 5 mM
- 0.2891 mL
- 1.4455 mL
- 2.8909 mL
- 10 mM
- 0.1445 mL
- 0.7227 mL
- 1.4455 mL

技术信息

CAS号	N/A	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C30H41N7O8S2	运输	蓝冰
分子量	691.82	别名	AZD9291 Dimesylate; Mereletinib Dimesylate

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