|N1-[2-(二甲基氨基)乙基]-5-甲氧基-N1-甲基-N4-[4-(1-甲基-1H-吲哚-3-基)-2-嘧啶基]-1,2,4-苯三胺|CsnPharm

CAS No.: 1421372-66-8

N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine Catalog No. CSN16873

Synonyms: Osimertinib analog;AZD9291-DA;AZD9291DA HCl

Osimertinib DA is a desacryl analogue of Osimertinib, is an intermediate inhibitor of mutated EGFR, including L858R EGFR, Exonl9 deletion and T790M resistance mutant.

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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]
参考文献

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
- 2.2444 mL
- 11.2218 mL
- 22.4437 mL
- 5 mM
- 0.4489 mL
- 2.2444 mL
- 4.4887 mL
- 10 mM
- 0.2244 mL
- 1.1222 mL
- 2.2444 mL

技术信息

CAS号

1421372-66-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H31N7O

运输

蓝冰

分子量

445.56

别名

Osimertinib analog;AZD9291-DA;AZD9291DA HCl;AZD9291DA HCl salt;AZD9291-DA hydrochloride

溶解度

DMSO	74.0 mg/mL (166.1 mM)

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N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine Catalog No. CSN16873

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