Nilotinib hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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，可用于慢性骨髓性白血病的研究。

Nilotinib (AMN107) hydrochloride is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia.

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.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 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.

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.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.Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X) Dosage:40 mg/kg Administration:Oral gavage; daily; 4 weeks Result:Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.

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Autophagy

Autophagy

Autophagy | Bcr-Abl

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923288-95-3

565.98

C28H23ClF3N7O

>98% (HPLC)

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Cl.O=C(NC=1C=C(C=C(C1)C(F)(F)F)N2C=NC(=C2)C)C3=CC=C(C(=C3)NC=4N=CC=C(N4)C5=CN=CC=C5)C

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(-20℃)

With Ice Pack

≥ 2 years