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Nilotinib

CAS No. : 641571-10-0

MCE 国际站：Nilotinib

产品活性：Nilotinib是一种口服可用的具有抗肿瘤活性的 Bcr-Abl 酪氨酸激酶抑制剂。

研究领域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点：Bcr-Abl  |  Autophagy

In Vitro: Nilotinib (AMN107), selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC₅₀<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance.
Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC₅₀ of 4.59±0.97 µM and 11.15±1.48 µM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC₅₀ values of 11.74±0.17 µM (P<0.001) and 41.37±1.07 µM (P<0.001), respectively.

In Vivo: Nilotinib (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft.
Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon.

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