Entrectinib恩曲替尼,1108743-60-7

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Entrectinib

CAS No. : 1108743-60-7

MCE 国际站：Entrectinib

产品活性：Entrectinib (NMS-E628) 是口服有效的，可透过血脑屏障的，且具有中枢神经活性的 TrkA/B/C, ROS1 和 ALK 抑制剂，其 IC₅₀ 值分别为 1, 3, 5, 12 和 7 nM。Entrectinib 诱导癌细胞凋亡和周期停滞，具有抗肿瘤活性，还可减轻博来霉素诱导的小鼠肺纤维化。

研究领域：Protein Tyrosine Kinase/RTK  |  Neuronal Signaling  |  Autophagy

作用靶点：ROS Kinase  |  Trk Receptor  |  Anaplastic lymphoma kinase (ALK)  |  Autophagy

In Vitro: Entrectinib (100, 200, 400 nM; 24 h) alleviates TGF-β1-induced activation of mouse lung fibroblasts.
Entrectinib(100, 200, 400 nM; 24 h) inhibits TGF-β1-induced epithelial to mesenchymal transition of mouse lung epithelial cells.
Entrectinib (10, 50, 250 nM; 2 h) abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCg1, AKT, and MAPK in KM12 cells.
Entrectinib (10, 50, 250 nM; 24, 48 h) induce KM12 cells cycle arrest (24 h) and apoptosis (48 h).

In Vivo: Entrectinib (20, 40, 60 mg/kg; i.g.; single daily for 7 days) attenuates bleomycin-induced pulmonary fibrosis in mice.
Entrectinib (30, 60 mg/kg; p.o.; twice daily for 10 consecutive days) induces regression of xenograft tumors in tumor-bearing mice, including TRKA-dependent colorectal cancer KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including brain-localized lung model cancer metastasis.

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