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Nilotinib hydrochloride

CAS No. : 923288-95-3

MCE 站：Nilotinib hydrochloride

产品活性：Nilotinib (AMN107) hydrochloride 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

作用靶点：Bcr-Abl  |  Autophagy

In Vitro: Nilotinib hydrochlorid, 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 hydrochlorid 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 M ａnd 11.15±1.48 M, respectively, imatinib-resistant cell lines GK1C-IR ａnd GK3C-IR shows 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: Nilotinib hydrochlorid (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft.
Nilotinib hydrochlorid 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：Dasatinib  |  Nocodazole  |  Imatinib  |  Ponatinib  |  Nilotinib  |  Bosutinib  |  Asciminib  |  Degrasyn  |  Rebastinib  |  AT9283  |  Olverembatinib  |  KW-2449  |  Bafetinib  |  LXH254  |  DPH  |  Flumatinib  |  PD173955  |  GNF-7  |  Vodobatinib  |  XL228  |  AST 487  |  Cenisertib  |  GNF-2  |  CZC-8004  |  SIAIS178

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