Orally active inhibitor of ALK kinase
CAS：1108743-60-7
分子式：C31H34F2N6O2
分子量：560.64
纯度：98%
存储：Store at -20°C

Background:

The receptor tyrosine kinases (RTKs) play a critical role, controlling cell proliferation, survival, and differentiation of normal cells. The anaplastic lymphoma kinase (ALK), a transmembrane RTK, originally identified in the nucleophosmin (NPM)–ALK chimera of anaplastic large cell lymphoma, has emerged as a novel tumorigenic player in several human cancers. Entrectinib is an orally available small-molecule inhibitor of ALK kinase activity.

In vitro: Entrectinib potently and selectively inhibits the in vitro growth of ALK-driven tumors, with confirmed mechanism of action [1].

In vivo: Since Entrectinib is able to pass the blood-brain barrier, the compound was also tested for efficacy in an xenograft model with ALK positive NSCLC tumors. MRI imaging demonstrated that Entrectinib was able to effectively and control the growth of these intracranial tumors dose-dependently, leading to increased survival [1].

Clinical trial: Entrectinib is an orally available small-molecule inhibitor of ALK kinase activity that is being evaluated in phase I/II clinical study to treat solid cancer

Reference:
[1] Elena Ardini, Maria Menichincheri, Patrizia Banfi, Daniele Casero, M. Laura Giorgini, M. Beatrice Saccardo, Nadia Amboldi, Nilla Avanzi, Paolo Orsini, Antonella Isacchi, Enrico Pesenti, Arturo Galvani. The ALK inhibitor NMS-E628 also potently inhibits ROS1 and induces tumor regression in ROS-driven models. [abstract]. In: Proceedings of the 104th Annual Meeting of the American Association for Cancer Research; 2013 Apr 6-10; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2013;73(8 Suppl):Abstract nr 2092. doi:10.1158/1538-7445.AM2013-2092
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