Mobocertinib succinate
(Synonyms: 莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate) 目录号 : GC62160
An inhibitor of mutant EGFR and HER2 receptors
Cas No.:2389149-74-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mobocertinib is an inhibitor of mutant EGFR and HER2 receptors.1,2 It is selective for the HER2 exon 20 mutants HER2V659E, HER2G660D, HER2G309E, and HER2S310F over wild-type EGFR in Ba/F3 cells.1
1.Chouitar, J., Vincent, S., Brake, R., et al.TAK-788 is a novel and potent tyrosine kinase inhibitor with selective activity against EGFR/HER2AbstractsS811P2(13-32)(2018) 2.Neal, J., Doebele, R., Riely, G., et al.Safety, PK, and preliminary antitumor activity of the oral EGFR/HER2 exon 20 inhibitor TAK-788 in NSCLCAbstractsS599P1(13-44)(2018)
| Cas No. | 2389149-74-8 | SDF | |
| 别名 | 莫博替尼琥珀酸盐; TAK-788 succinate; AP32788 succinate | ||
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4209 mL | 7.1045 mL | 14.209 mL |
| 5 mM | 0.2842 mL | 1.4209 mL | 2.8418 mL |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4209 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Discovery, Development, Inventions, and Patent Trends on Mobocertinib succinate: The First-in-Class Oral Treatment for NSCLC with EGFR Exon 20 Insertions
Biomedicines 2021 Dec 17;9(12):1938.PMID:34944754DOI:10.3390/biomedicines9121938.
The majority of lung cancers are non-small-cell lung cancer (NSCLC) having a low survival rate. Recent studies have indicated the involvement of epidermal growth factor receptor (EGFR) oncogene mutations like EGFR exon 20 insertions (EGFRex20ins) mutation among NSCLC patients. The response of patients of NSCLC with the EGFRex20ins mutation to the currently available EGFR inhibitor is negligible. Mobocertinib is the first oral treatment that has been approved by the USFDA, on 15 September 2021, to treat NSCLC with the EGFRex20ins mutation. This patent review discusses the inventions and patent literature of mobocertinib that will help the scientific community to develop additional and improved inventions related to mobocertinib. The structure of mobocertinib was first reported in 2015. Therefore, this article covered the patents/patent applications related to mobocertinib from 2015 to 25 October 2021. The patent search revealed 27 patents/patent applications related to compound, method of treatment, salt, polymorph, process, composition, and drug combinations of mobocertinib. The authors foresee an exciting prospect for developing a treatment for NSCLC with EGFRex20ins mutation, and other cancers employing a combination of mobocertinib with other approved anticancer agents. The inventions related to novel dosage forms, processes, and intermediates used in the synthesis of mobocertinib are also anticipated.