Nilotinib (AMN-107)

For research use only. Not for use in humans.

目录号:S1033 中文名称:尼洛替尼

Nilotinib (AMN-107) Chemical Structure

CAS No. 641571-10-0

Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂,在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 749.92 现货
RMB 810.81 现货
RMB 1040.13 现货
RMB 1720.01 现货
RMB 3005.73 现货
RMB 3864.35 现货
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客户使用Selleck生产的Nilotinib (AMN-107)发表文献122篇:

产品安全说明书

Bcr-Abl抑制剂选择性比较

生物活性

产品描述 Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂,在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。
特性 Nilotinib 是Abl选择性抑制剂,与BCR-ABL的ATP结合位点相互作用。
靶点
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
体外研究

Nilotinib 作用于激活的HSCs,抑制增殖,迁移,和肌动蛋白形成,及 α-SMA和胶原的表达。Nilotinib 诱导HSCs凋亡,与bcl-2 表达降低相关,且提高p53 表达, PARP分裂,以及提高 PPARγ 和TRAIL-R表达。Nilotinib 也诱导细胞周期停滞,伴随着p27 的表达和cyclin D1的下调提高。Nilotinib 不仅抑制PDGFR的激活,也 通过Src抑制TGFRII。Nilotinib 显著抑制PDGF和 TGFβ刺激的ERK 和Akt磷酸化。而且, Nilotinib作用于人HSCs,抑制PDGF和TGFβ-激活的Abl磷酸化形式。 [2]Nilotinib抑制最抗 Imatinib的BCR-ABL突变,除了T315I。[3] Nilotinib 抑制PDGF-DD调节的 ERK1/2激活,基本的和PDGF-DD调节的 PDGFR-β和AKT激活,及schwannoma细胞增殖。 Nilotinib 比Imatinib更有效,发挥其最大抑制效果时的浓度比稳态血浆水平还低。[4] Nilotinib也显著降低TGF-β1和血小板衍生的生长因子(PDGF)基因表达水平。Nilotinib处理也显著抑制PDGF诱导的肺纤维细胞增殖。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell NUjLTnNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHPXZlKSzVyPUCuNFAxOTR2IN88US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
KU812 M4PydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml34TWM2OD1yLkCwNlQ5KM7:TR?= NXGzWHJjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
EM-2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjoW5BKSzVyPUCuNFA1OSEQvF2= NEDacJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
LAMA-84 M2\yZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTtTWM2OD1yLkCwOFkh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
MEG-01 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;UboJZUUN3ME2wMlAxQDJ6IN88US=> MlPNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
BV-173 NGroTplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fMfmlEPTB;MD6wNVA5QSEQvF2= NXHqTmRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
KASUMI-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELIb4JKSzVyPUCuNFI1OTNizszN NFr6Nlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
NB7 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHviO4pKSzVyPUCuNVM1OzlizszN M1rSfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
BHT-101 Mo\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNkSyOlMh|ryP MkLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
CGTH-W-1 NFHuU3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DYcmlEPTB;MD62OFg4KM7:TR?= NYX0SoNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
HMV-II MmjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfXVJRWUUN3ME2wMlc1QDd2IN88US=> MmTNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
NKM-1 NXHPNXFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXEO4lWUUN3ME2wMlkxOTVizszN MoLCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
LB2241-RCC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzpTWM2OD1zLkCyNlI5KM7:TR?= M3vrVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
NCI-H1703 NWTLVGJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTFwMUi4O{DPxE1? NYHVcXRIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
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HOP-62 NXj3fI9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;xbWlEPTB;MT64NlA4PyEQvF2= NH6y[mc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
H9 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TsWWlEPTB;Mj63N|c6OyEQvF2= M1O4XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
HCC1806 M1\CU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrqT|FKSzVyPUKuO|Q{OjdizszN NEDUWoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
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RS4-11 NVnoelI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmK2TWM2OD1{LkmwOlI{KM7:TR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
JAR NWXrfGJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvwUoZLUUN3ME2yMlkzODh2IN88US=> NUTl[3NvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
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NCI-SNU-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNwNECwPVIh|ryP NHLxWZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
SK-MEL-1 NHP4d3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHKdJVKSzVyPUOuOFMxOjlizszN NIS3bHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
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SW982 MkTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjzPYM4UUN3ME2zMlY1OTZ7IN88US=> NEjuc4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
HT-1080 NGTqWoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L1c2lEPTB;Mz65NVc4PSEQvF2= Mo\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
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HOS MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j5emlEPTB;ND64NFI5OiEQvF2= M2e3T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
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HAL-01 Moq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPr[nRzUUN3ME20Mlg5OjR{IN88US=> M3XmN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
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LCLC-103H NIj6ToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjRUYNZUUN3ME21Mlc4PDdzIN88US=> NH7kOpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ ; 

PubMed: 23677989     


Dose-dependent analysis of AMPK-related molecules in HCC cells. Cells were exposed to nilotinib at the indicated concentrations for 24 h.

DNMT1 / DNMT3a / DNMT3b ; 

PubMed: 28720666     


Kasumi-1 or MV4-11 cells were treated for 24 h with the indicated doses of nilotinib and subjected western blot analysis to detect the expression levels of DNMT1, DNMT3a, DNMT3b.

pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 ; 

PubMed: 31396300     


ABL1 regulated the inflammation signaling pathway. Blocking activities of ABL1 with Imatinib and Nilotinib inhibits the inflammatory signaling pathway including activities of NF-κB1, STAT3, IL-1β, IL-6, and COX2.

23677989 28720666 31396300
Growth inhibition assay
Cell viability; 

PubMed: 23677989     


Dose-dependent effects of nilotinib on cell viability. HCC cells were treated with nilotinib at the indicated concentrations for 72 h. Cell viability was measured by MTT assay. Points, mean; bars, S.D. (n = 8). 

23677989
体内研究 Nilotinib 作用于CCl4和BDL诱导的纤维化,降低胶原沉积和α-SMA表达。 Nilotinib 可以诱导HSC发生凋亡,与bcl-2的下调相关。 [2] Nilotinib轻肺损伤和纤维化程度。Nilotinib 疗法在第14天和21天,显著降低羟脯氨酸水平 ,伴随着转化生长因子(TGF)-β1和 PDGFR-β表达水平降低。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[4]
- 合并
  • Cell lines: 人类原代Schwann 和schwannoma细胞
  • Concentrations: 1 μM -10 μM
  • Incubation Time: 72小时
  • Method: 人类原代 Schwann和 schwannoma细胞接种在预包被的96孔板上。加入Nilotinib,40分钟后,使用100 ng/mL PDGF-DD刺激处理,细胞培养72小时(3 天)。因为Nilotinib的半衰期为18小时, 每天新鲜补充的浓度为最初加入浓度的一半。除了DAPI染色和测定全部细胞数外, 使用更敏感和准确的 BrdU渗透法测定增殖细胞。 使用倒置荧光显微镜和200 ×放大倍率。计算全部细胞数(DAPI)和分裂细胞数(BrdU阳性)。计数每孔中的所有细胞。每孔中不同批次细胞的全部细胞数不同。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 雄性6周大的C57BL6小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 27 mg/mL (50.98 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
3mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 529.52
化学式

C28H22F3N7O

CAS号 641571-10-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05185947 Not yet recruiting Drug: Paclitaxel|Drug: Nilotinib Peritoneal Carcinomatosis|Peritoneal Neoplasms|Ovarian Cancer|Ovarian Neoplasms|Colorectal Cancer|Colorectal Neoplasms|Appendiceal Cancer|Appendiceal Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 18 2022 Phase 2
NCT04326933 Not yet recruiting Drug: Tyrosine kinase Inhibitors (Imatinib & Nilotinib) Patients Diagnosed as Chronic Meyloid Leukemia Assiut University October 20 2020 --
NCT04002674 Recruiting Drug: Placebo oral capsule|Drug: Nilotinib Oral Capsule Dementia With Lewy Bodies Georgetown University|National Institutes of Health (NIH) January 10 2020 Phase 2
NCT03942094 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Chronic Phase|Nilotinib Shenzhen Second People''s Hospital|Zhongshan City People''s Hospital|Affiliated Hospital of Guangdong Medical University|Huazhong University of Science and Technology Union Shenzhen Hospital|Dongguan People''s Hospital|Longgang District Central Hospital of Shenzhen June 1 2019 Phase 3

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常见问题及建议解决方法

  • 问题 1:

    I would like to use AMN-107 for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

  • 回答:

    For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml.

Bcr-Abl Signaling Pathway Map

Bcr-Abl Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID