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尼罗替尼 (AMN-107)

高效选择性Bcr / Abl酪氨酸激酶抑制剂
规格或纯度: ≥99%
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货号 (SKU) 包装规格 是否现货 价格 数量
N126111-25mg
 25mg 现货 Stock Image
N126111-100mg
 100mg 现货 Stock Image
N126111-250mg
 250mg 现货 Stock Image
N126111-1g
 1g 现货 Stock Image
N126111-5g
 5g 现货 Stock Image
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ABL proto-oncogene 1，non-receptor tyrosine kinase Inhibitor discoidin domain receptor tyrosine kinase 1 Inhibitor discoidin domain receptor tyrosine kinase 2 Inhibitor
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基本描述

规格或纯度 ≥99%
英文名称 Nilotinib (AMN-107)
别名 尼罗替尼|尼洛替尼
英文别名 Nilotinib|641571-10-0|Tasigna|AMN107|AMN 107|AMN-107|nilotinibum|Nilotinib free base|Nilotinib (AMN-107)|NSC-747599|4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide|4-methyl-N-[3-(4-met
生化机理 Nilotinib is a small molecule Bcr-Abl kinase inhibitor, rationally designed to bind and inhibit the c-Abl kinase active site with more affinity than the prototypic Bcr-Abl kinase inhibitor Imatinib (sc-202180). Nilotinib demonstrates a high affinity for the kinase (IC50 < 30nM) and shows efficacy against chronic myelogenous leukemias (CML) expressing the Bcr-Abl oncogene/fusion protein, both the wild type and CMLs presenting Imatinib resistance. .Potent and selective Bcr/Abl tyrosine kinase inhibitor (IC 50 = 15 nM). JAK2/STAT5 inhibitor. Inhibits MDM2 at the post-translational level by inducing MDM2 self-ubiquitination and degradation. Shows antiproliferative and antitumor effects in vivo .
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

Nilotinib (尼洛替尼; AMN-107) 是Bcr-Abl抑制剂，IC50小于30 nM。A rationally designed c-Abl and Bcr-Abl kinase inhibitor


一般描述

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。

Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM.
A rationally designed c-Abl and Bcr-Abl kinase inhibitor

名称和标识符

IUPAC Name 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
INCHI InChI=1S/C28H22F3N7O/c1-17-5-6-19(10-25(17)37-27-33-9-7-24(36-27)20-4-3-8-32-14-20)26(39)35-22-11-21(28(29,30)31)12-23(13-22)38-15-18(2)34-16-38/h3-16H,1-2H3,(H,35,39)(H,33,36,37)
InChi Key HHZIURLSWUIHRB-UHFFFAOYSA-N
Canonical SMILES CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
PubChem CID 644241
分子量 529.53

化学和物理性质

溶解性 DMSO ≥10mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
密度 1.36
折光率 1.65
熔点 230-242℃

安全和危险性（GHS）

象形图
ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H373: Causes damage to organs through prolonged or repeated exposure
H413: May cause long lasting harmful effects to aquatic life
H400: Very toxic to aquatic life
H410: Very toxic to aquatic life with long lasting effects
H372: Causes damage to organs through prolonged or repeated exposure
H360: May damage fertility or the unborn child
H361: Suspected of damaging fertility or the unborn child
预防措施声明 P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P260,P270,P362+P364,P391,P203,P264+P265,P318,P337+P317,P332+P317,P319

关联配体

Ligand ID 5697
名称 nilotinib
别名 AMN107
类别 Synthetic organic
学名 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide
生物活性评价 Off-targets include KIT, PDGFRA and PDGFRB.
评价 Nilotinib is a Type-2 kinase inhibitor and was first approved by the FDA in 2007.
Preclinical studies in rodent Parkinson's disease models suggest that nilotinib has some potential to promote autophagic degradation of α-synuclein , a brain protein whose accumulation and aggregation contributes to the formation of toxic insoluble fibrils which cause pathological changes such as neuronal loss in Parkinson's disease and other synucleinopathies. This mechanism has been evaluated in a pilot, proof-of-concept and safety clinical trial in a small number of patients with Parkinson's disease- and diffuse Lewy body disease-associated cognitive impairment (see NCT02281474; note that this trial is not placebo controlled or blinded).

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参考文献

1. Hebron ML, Lonskaya I, Moussa CE.  (2013)  Nilotinib reverses loss of dopamine neurons and improves motor behavior via autophagic degradation of α-synuclein in Parkinson's disease models..  Hum Mol Genet,  22  (16):  (3315-28).  [PMID:23666528]
2. Hebron ML, Lonskaya I, Moussa CE.  (2013)  Tyrosine kinase inhibition facilitates autophagic SNCA/α-synuclein clearance..  Autophagy,  9  (8):  (1249-50).  [PMID:23787811]
3. Tanabe A, Yamamura Y, Kasahara J, Morigaki R, Kaji R, Goto S.  (2014)  A novel tyrosine kinase inhibitor AMN107 (nilotinib) normalizes striatal motor behaviors in a mouse model of Parkinson's disease..  Front Cell Neurosci,  8  (13):  (50).  [PMID:24600352]
4. Karuppagounder SS, Brahmachari S, Lee Y, Dawson VL, Dawson TM, Ko HS.  (2014)  The c-Abl inhibitor, nilotinib, protects dopaminergic neurons in a preclinical animal model of Parkinson's disease..  Sci Rep,  4  (13):  (4874).  [PMID:24786396]
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