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Nilotinib hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nilotinib hydrochloride图片
CAS NO:923288-95-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AMN107 hydrochloride
产品介绍
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。
生物活性

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].

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

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].

Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
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.
Clinical Trial
分子量

565.98

Formula

C28H23ClF3N7O

CAS 号

923288-95-3

中文名称

盐酸尼洛替尼;盐酸尼罗替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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