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Nilotinib

產(chǎn)品活性：Nilotinib是一種口服可用的具有抗腫瘤活性的 Bcr-Abl 酪氨酸激酶抑制劑。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK  |  Autophagy

作用靶點(diǎn)：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.

相關(guān)產(chǎn)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  |  Drug Repurposing Compound Library  |  NMPA-Approved Drug Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Alzheimer's Disease Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Therapy Drug Library   |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Human Metabolite Library  |  Heterocyclic Compound Library  |  Withdrawn Drug Compound Library  |  SNIPER(ABL)-013  |  AT9283  |  Bafetinib  |  Flumatinib mesylate  |  Olverembatinib  |  GNF-2  |  BCR-ABL-IN-6  |  Ponatinib hydrochloride  |  GNF-5  |  Vamotinib  |  CT-721  |  ON 146040  |  Bosutinib hydrate  |  Ponatinib-d₈  |  Imatinib-d₈  |  GMB-475  |  BCR-ABL-IN-5  |  Dasatinib monohydrate  |  Imatinib-d₄  |  Debio 0617B  |  Nilotinib monohydrochloride monohydrate  |  SNIPER(ABL)-049  |  SNIPER(ABL)-033  |  KW-2449  |  Imatinib-d₃ (hydrochloride)  |  CHMFL-ABL-039  |  SNIPER(ABL)-050  |  BCR-ABL1-IN-1

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