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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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Blood Cancer Compound Library  |  Nocodazole  |  Imatinib  |  Bosutinib  |  AT9283  |  KW-2449  |  Bafetinib  |  DPH  |  AST 487  |  PD173955  |  GNF-7  |  GNF-5  |  GMB-475  |  GNF-2  |  Lyn-IN-1  |  DB07107  |  SNIPER(ABL)-020  |  CHMFL-ABL/KIT-155  |  CT-721  |  Imatinib D4  |  Imatinib D8  |  Multi-kinase inhibitor 1  |  ON 146040  |  PD180970  |  Pivanex  |  PROTAC BCR-ABL1 ligand 1  |  BCR-ABL-IN-1  |  SNIPER(ABL)-013  |  SNIPER(ABL)-015

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