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抑制剂 > JAK STAT信令 > Mobocertinib succinate
产品名称:
Mobocertinib succinate
型号:
CS-01Y78457
生产地址
国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10 mg 25 mg 50 mg 100 mg 500 mg

CAS

2389149-74-8

别名

N/A

化学名

N/A

分子式

C36H45N7O8

分子量

703.78

溶解度

DMSO : 25 mg/mL (35.52 mM; Need ultrasonic)

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity[1][2].

Mobocertinib succinate (TAK-788 succinate) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM), including all 8 variants with exon 20 activating insertions[1].

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, once daily oral dosing of Mobocertinib succinate induced regression of tumors at doses that were well tolerated (30-100 mg/kg)[1].

[1]. Francois Gonzalvez, et al. Abstract 2644: AP32788, a potent, selective inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, in preclinical models. April 16-20, 2016; New Orleans, LA.

[2]. Masood A, et al. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on BIBW 2992. Semin Oncol. 2019 Jun;46(3):271-283.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Mobocertinib succinate 

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