Nilotinib (AMN107) hydrochloride is an orally activeBcr-Abltyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia^[1][2][3].

Nilotinib hydrochloride, 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^[1].
Nilotinib hydrochloride 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 IC₅₀of 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 IC₅₀values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively^[2].

Nilotinib hydrochloride (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft^[2].
Nilotinib hydrochloride 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^[3].

565.98

C₂₈H₂₃ClF₃N₇O

923288-95-3

盐酸尼洛替尼；盐酸尼罗替尼

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.