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抑制剂/激动剂
囊泡 肿瘤
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血管生成
TGF-beta/Smad 蛋白质酪氨酸激酶 干细胞 外泌体 肿瘤干细胞 Notch
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Bcr-Abl
转化生长因子-β
/ Nilotinib

尼洛替尼 /Nilotinib {[allProObj[0].p_purity_real_show]}

货号：A448494 同义名： 尼罗替尼 (AMN-107) / AMN107

Nilotinib是一种口服可用的Bcr-Abl酪氨酸激酶抑制剂，具有抗肿瘤特性。

Nilotinib 化学结构 CAS号：641571-10-0
Nilotinib 化学结构
CAS号：641571-10-0
Nilotinib 3D分子结构
CAS号：641571-10-0
Nilotinib 化学结构 CAS号：641571-10-0
Nilotinib 3D分子结构 CAS号：641571-10-0
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Nilotinib 纯度/质量文件 产品仅供科研

货号：A448494 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Abl ↓ Bcr-Abl ↓ 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

 		99%+
KW-2449 +++

Abl, IC50: 14 nM

Abl (T315I), IC50: 4 nM

 		FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

 		98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

 		c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

 		RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

 		FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

 		PDGFR,VEGFR 99%+
GNF-7 +++

E255V, IC50: 122 nM

M351T, IC50: 133 nM

 		99%+
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

 		99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

 		Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

 		Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

 		98+%
GNF-2 +

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

Bcr-Abl (K562 cell line), IC50: 273 nM

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		98%
Radotinib ++

BCR-ABL1, IC50: 34 nM

 		98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
SIS3 ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		98%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Nilotinib 生物活性

靶点

  • Bcr-Abl

    Bcr-Abl, IC50:<30 nM
描述 The oncogenic tyrosine kinase Bcr-Abl plays a central role in the pathogenesis of chronic myelogenous leukemia, thus makes it as the therapy drug target. However, it is demonstrated that the mutations of Bcr-Abl kinase have been the most common mechanism of drug resistance, such as imatinib. Nilotinib is a potent and selective Bcr-Abl inhibitor with IC50 values of 15nM, as well as IC50 values ranging in 9-400nM for different Abl mutations except the T315l mutation (measured by in vitro kinase assays)[1]. Though Nilotinib was structured based on imatinib, in vitro study showed that Nilotinib showed differential sensitivity of Abl point mutations with imatinib[1][2]. Nilotinib inhibited proliferation of Ba/F3 cells expressing G250E, E255K(V), F317L, M351T, F486S, M244V, L248R, Q252H, Y253H, E255K, E279K, E282D, V289S, and L348M Bcr-Abl mutants at concentration<1μM, as well as tyrosine autophosphorylation of the E255K, E255V, F317L, M351T and F486S Bcr-Abl mutants with mean IC50 values of 150, 246, 41, 31 and 43 nM, respectively. Activity against PDGFR and c-Kit by Nilotinib also can be observed at concentration<200nM. Oral dose of 75mg/kg Nilotinib prolonged survival and decreased tumor burden in an imatinib-resistant Bcr-Abl mutant BMT model[2].
作用机制 Nilotinib was found to bind to the inactive conformation of Abl as observed for imatinib, resulting differential sensitivity of Abl point mutations by Nilotinib.[2]

Nilotinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=11.2101 μM SANGER
769-P Growth Inhibition Assay IC50=19.6335 μM SANGER
A101D Growth Inhibition Assay IC50=10.8923 μM SANGER
A172 Growth Inhibition Assay IC50=25.7136 μM SANGER

Nilotinib 动物研究

Dose Rat: 5 mg/kg - 40 mg/kg[3] (p.o.) Mice: 30 mg/kg - 300 mg/kg[3] (p.o.), 10 mg/kg[4] (i.p.)
Administration p.o., i.p.

Nilotinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00785785 - Completed - -
NCT01220648 Chronic Myeloid Leukemia Phase 1 Completed - Germany ... 展开 >> Novartis Investigative Site Leipzig, Germany, 04103 收起 <<
NCT01806571 Untreated Adult Acute Myeloid ... 展开 >>Leukemia 收起 << Phase 2 Active, not recruiting April 18, 2020 United States, Arizona ... 展开 >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<

Nilotinib 参考文献

[1]O'Hare T, Walters DK, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500-5.

[2]Weisberg E, Manley PW, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41.

Nilotinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.44mL

1.89mL

0.94mL

18.89mL

3.78mL

1.89mL

Nilotinib 技术信息

CAS号641571-10-0
分子式C28H22F3N7O
分子量 529.52
别名 尼罗替尼 (AMN-107) ;AMN107
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 12 mg/mL(22.66 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+water 0.2 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: Nilotinib | AMN107 | 尼罗替尼 (AMN-107) | Bcr-Abl | TGF-beta/Smad | AmBeed-信号通路专用抑制剂 | Nilotinib 纯度/质量文件 | Nilotinib 亚型比较 | Nilotinib 生物活性 | Nilotinib 细胞研究 | Nilotinib 动物研究 | Nilotinib 临床数据 | Nilotinib 参考文献 | Nilotinib 实验方案 | Nilotinib 技术信息

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