|N-(3-((2-((3-氟-4-(4-甲基哌嗪-1-基)苯基)氨基)-7H-吡咯并[2,3-d]嘧啶-4-基)氧基)苯基)丙烯酰胺马来酸盐|CsnPharm

CAS No.: 1557268-88-8

艾维替尼马来酸盐 Catalog No. CSN20602

Synonyms: Abivertinib maleate;AC0010 maleate;AC-0010MA

Avitinib maleate, the maleate salt form of avitinib, selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate.

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实验方案

技术信息

生物活性

描述Avitinib Maleate is the maleate form of Avitinib.Avitinib is an irreversible EGFR inhibitor selectively targeting mutated EGFR active and T790M mutations with IC50 value of 0.18nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50=7.68nM), in the kinase enzymatic assay. AC0010 potently inhibited cellular EGFR-Tyr1068 phosphorylation with IC50 value of 4.4nM and 9.8nM in NCIH1975 cells and HCC827 cells, respectively, accompanied with inhibited phosphorylation of the downstream targets Akt and ERK1/2. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR-active and T790M mutations for over 143 days with no weight loss^[2].
作用机制Avitinib covalently modifies recombinant EGFR T790M mutation at the target cysteine 797 amino acid.^[1]
动物研究
剂量
Mice: 12.5 mg/kg - 500 mg/kg^[1] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 12.5 mg/kg - 500 mg/kg^[1] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02274337	Non-Small Cell Lung Cancer	Phase 1 Phase 2	Unknown	December 2017	China, Guangdong ... more >> Sun Yat-Sen University Cancer Center Recruiting Guangzhou, Guangdong, China, 510060 Contact: Yuxiang Ma, MD 86-020-87343894 mayx@sysucc.org.cn Collapse <<
NCT03574402	Carcinoma, Non-Small-Cell Lung	Phase 2	Not yet recruiting	December 30, 2024	-

参考文献

[1] Xu X, Mao L, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597. Epub 2016 Aug 29.
[2] Xu X, Mao L, Xu W, Tang W, Zhang X, Xi B, Xu R, Fang X, Liu J, Fang C, Zhao L, Wang X, Jiang J, Hu P, Zhao H, Zhang L. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597. doi: 10.1158/1535-7163.MCT-16-0281. Epub 2016 Aug 29. PMID: 27573423.

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
- 1.6567 mL
- 8.2836 mL
- 16.5672 mL
- 5 mM
- 0.3313 mL
- 1.6567 mL
- 3.3134 mL
- 10 mM
- 0.1657 mL
- 0.8284 mL
- 1.6567 mL

技术信息

CAS号

1557268-88-8

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

C30H30FN7O6

运输

蓝冰

分子量

603.60

别名

Abivertinib maleate;AC0010 maleate;AC-0010MA;AC-0010;艾维替尼马来酸盐

溶解度

DMSO	100.0 mg/mL (165.7 mM)

动物实验配方

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