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Nilotinib monohydrochloride monohydrate

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产品价格:电议      采购度:1588      原产地:美洲

发布时间:2021/8/2 15:25:52      所属地区:上海 上海市

简要描述:

Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制 BCR-ABL 及其突变体。

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Nilotinib monohydrochloride monohydrate

CAS No. : 923288-90-8

MCE 站:Nilotinib monohydrochloride monohydrate

产品活性:Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制 BCR-ABL 及其突变体。

研究领域:Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶点:Bcr-Abl  |  Autophagy

In Vitro: The novel, selective Abl inhibitor, Nilotinib (AMN107), is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than Imatinib. In addition to being significantly more potent compared with Imatinib (IC50<30 nM), Nilotinib 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. The parent cell lines GK1C and GK3C show Imatinib sensitivity with IC50 of 4.59±0.97 ?M and 11.15±1.48 ?M, respectively. The Imatinib-resistant cell lines GK1C-IR and GK3C-IR show Imatinib resistance with IC50 values of 11.74±0.17 ?M (P<0.001) and 41.37±1.07 ?M (P<0.001), respectively.

In Vivo: The percentage of tumor growth inhibition (TGI) is 83.8% for Imatinib and 69.6% for Nilotinib in the GK1X xenograft line (n.s.). In the GK2X xenograft line, TGI is 83.0% for Imatinib and 85.3% for Nilotinib (n.s.). Additionally, the GK3X xenograft line TGI is 31.1% for Imatinib and 47.5% for Nilotinib (n.s.). These results suggest that, except for the GK1X xenograft line, Nilotinib shows equivalent or higher antitumor effects than Imatinib. 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 Nilotinib decreased the PDGFR α and β levels and apoptotic scores in the colon, it did not have a significant effect on the weight and TNF-α levels. Further experimental investigations could provide more definitive evidence for humans.

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更新时间:2024/1/2 10:17:29

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