尼罗替尼.|641571-10-0|(尼洛替尼; AMN107)-陌孚医药/Medlife

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尼罗替尼. (Synonyms: 尼洛替尼; AMN107)

目录号: PC10003 纯度: >99%

CAS No. :641571-10-0

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中文名称

尼罗替尼.

中文别名

尼罗替尼及其中间体;4-甲基-3-((4-(3-吡啶基)-2-嘧啶基)氨基)-N-(5-(4-甲基-1H-咪唑-1-基)-3-(三氟甲基)苯基)苯甲酰胺;尼罗替尼;Nilotinib (AMN-107) 抑制剂;尼罗替尼尼洛替尼;尼罗替尼标准品;尼罗替尼碱;尼洛替尼;4-甲基-3-((4-(3-吡啶基)-2-嘧啶基)氨基)-N-(5-(4-甲基-1H-咪唑-1-基)-3-(三氟甲基)苯基)苯甲酰;NILO锡IB;苯甲酰胺, 4-甲基-N-[3-(4-甲基-1H-咪唑-1-基)-5-(三氟甲基)苯基]-3-[[4-(3-吡啶基)-2-嘧啶基]氨基];尼罗替尼

英文名称

Nilotinib

英文别名

Nilotinib;AMN 107;Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-;4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4 -pyridin-3-ylpyrimidin-2-yl)amino]benzamide Nilotinib(TINIBS );4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide;Nilotinib for research;Tasigna;Nilotinib &its intermediates (Developing);Nilotinib (AMN-107);4-Methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)-phenyl)-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)benzamide;Benzamide, 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyrid...;Nilotinib (AMN-107,Tasigna®);Nilotinib(AMN 107);Posaconazole inter; Afatinib;AMN-107;BIBW2992;its intermediates;Nilotinib,AMN107,Tasigna;TASIGNA NILOTINIB;Nilotinib & its intermediates;Nilotinib & its intermediates;AMN107;4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide;C28H22F3N7O;HHZIURLSWUIHRB-UHFFFAOYSA-N;NSC747599;4-Methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl

Cas No.

641571-10-0

分子式

C₂₈H₂₂F₃N₇O

分子量

529.52

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

性状

Solid

IC50 & Target[1][2]

Bcr-Abl

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20. [Information]

[2]. Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613. [Information]

[3]. Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85. [Information]

[4]. Fujita KI, et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. J Pharm Sci. 2017 Sep;106(9):2632-2641. [Information]

[5]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Information]

溶解度数据

体外研究:

DMSO : 12.5 mg/mL (23.61 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8885 mL	9.4425 mL	18.8850 mL
5 mM	0.3777 mL	1.8885 mL	3.7770 mL
10 mM	0.1889 mL	0.9443 mL	1.8885 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.5 mg/mL (0.94 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (0.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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