|2-((5-丙烯酰胺基-4-((2-(二甲基氨基)乙基)(甲基)氨基)-2-甲氧基苯基)氨基)-4-(1-甲基-1H-吲哚-3-基)嘧啶-5-羧酸异丙酯|CsnPharm

CAS No.: 1847461-43-1

莫博替尼 Catalog No. CSN26124

Synonyms: 莫博替尼;TAK-788;AP32788

TAK-788 is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. It is in a phase 1/2 open-label, multicenter study.

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

描述EGFR is a member of the ErbB family of structurally related RTKs (receptor tyrosine kinases), consisting of the EGFR (ErbB1), as well as human epidermal growth factor receptor 2 (ErbB2; HER2), ErbB3 (HER3) and ErbB4 (HER4). Aberrant ErbB family signaling is implicated in the development and progression of many human cancers, including NSCLC (non-small cell lung cancer)^[1]. Mobocertinib is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions. It inhibits wide-type EGFR with an IC₅₀ value of 35 nM and all 14 mutant variants of EGFR with IC₅₀s ranging from 2.4 to 22 nM, and all 6 mutant variants of HER2 with IC₅₀s ranging from 2.4 to 26 nM. In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, mobocertinib (once daily oral dosing at 30 - 100 mg/kg) induced regression of tumors^[2]. In a phaseI/II study of the EGFR/HER2 TKI, mobocertinib, in patients with advanced NSCLC refractory to standard therapy, the partial response (PR) rate was 21%, with 64% disease control rate^[1].
参考文献

[1] Masood A, Kancha RK, Subramanian J. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib. Semin Oncol. 2019;46(3):271-283
[2] AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models

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
- 1.7074 mL
- 8.5368 mL
- 17.0737 mL
- 5 mM
- 0.3415 mL
- 1.7074 mL
- 3.4147 mL
- 10 mM
- 0.1707 mL
- 0.8537 mL
- 1.7074 mL

技术信息

CAS号

1847461-43-1

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

C32H39N7O4

运输

蓝冰

分子量

585.70

别名

莫博替尼;TAK-788;AP32788

溶解度

DMSO	9.0 mg/mL (15.4 mM)
Water	Insoluble
Ethanol	Insoluble

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

莫博替尼 Catalog No. CSN26124

靶点选择性

请登录您的专属账户

确认信息