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

CAS No.: 1557267-42-1

Avitinib/艾维替尼 Catalog No. CSN20594

Synonyms: Abivertinib;AC0010

Avitinib selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR active mutations

IC50:7.68nM
描述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.^[2]
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
NCT03574402	Carcinoma, Non-Small-Cell Lung	Phase 2	Not yet recruiting	December 30, 2024	-
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 <<

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
- 2.0512 mL
- 10.2558 mL
- 20.5116 mL
- 5 mM
- 0.4102 mL
- 2.0512 mL
- 4.1023 mL
- 10 mM
- 0.2051 mL
- 1.0256 mL
- 2.0512 mL

技术信息

CAS号

1557267-42-1

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26FN7O2

运输

蓝冰

分子量

487.53

别名

Abivertinib;AC0010

溶解度

DMSO	97.0 mg/mL (199.0 mM)
Water	Insoluble
Ethanol	96.0 mg/mL (196.9 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Avitinib/艾维替尼 Catalog No. CSN20594

靶点选择性

请登录您的专属账户

确认信息