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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
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 | 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Drug Library | FDA-Approved Anticancer Drug Library | Human Metabolite Library | Heterocyclic Compound Library | Withdrawn Drug Compound Library | Cell Death Library | Anti-Hematopathy Compound Library | Bioactive Compound Library Max | Dasatinib | Nocodazole | Imatinib | Ponatinib | Bosutinib | Degrasyn | Asciminib | Olverembatinib | Rebastinib | AT9283 | Naporafenib | Bafetinib | KW-2449 | Nilotinib monohydrochloride monohydrate | BV02 | AST 487 | DPH | Flumatinib | XL228 | GNF-2 | PD173955 | GNF-7 | GNF-5 | Radotinib | Cenisertib
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