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| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N126111-25mg |
25mg |
现货 ![]() |
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| N126111-100mg |
100mg |
现货 ![]() |
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| N126111-250mg |
250mg |
现货 ![]() |
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| N126111-1g |
1g |
现货 ![]() |
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| N126111-5g |
5g |
现货 ![]() |
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| 别名 | 尼罗替尼 | 尼洛替尼 |
|---|---|
| 英文别名 | Nilotinib [USAN:INN:BAN] | 4-Methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide | AMN 107 Base Form | 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-{(4-(pyridin-3-y |
| 规格或纯度 | Moligand™, ≥99% |
| 英文名称 | Nilotinib (AMN-107) |
| 生化机理 | 尼罗替尼是一种小分子Bcr-Abl激酶抑制剂,经过合理设计,与原型Bcr-Abl激酶抑制剂伊马替尼(Imatinib,sc-202180)相比,它能以更高的亲和力结合并抑制c-Abl激酶活性位点。尼罗替尼对激酶具有很高的亲和力(IC50 < 30nM),对表达 Bcr-Abl 癌基因/融合蛋白的慢性骨髓性白血病(CML)(包括野生型和出现伊马替尼耐药的 CML)均有疗效。.强效、选择性 Bcr/Abl 酪氨酸激酶抑制剂(IC 50 = 15 nM)。JAK2/STAT5 抑制剂。通过诱导 MDM2 自我泛素化和降解,在翻译后水平抑制 MDM2。在体内具有抗增殖和抗肿瘤作用。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | ABL 原癌基因 1 抑制剂;非受体酪氨酸激酶;盘状结构域受体酪氨酸激酶 1 抑制剂;盘状结构域受体酪氨酸激酶 2 抑制剂 |
| 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 Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM. |
| 纯度 | ≥99% |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| PubChem SID | 504759766 |
|---|---|
| 分子类型 | 小分子 |
| IIUPAC Name | 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide |
| 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 |
| 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 |
| Isomeric 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 |
| 分子量 | 529.53 |
| Reaxy-Rn | 10737140 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=10737140&ln= |
| 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℃ |
| 分子量 | 529.500 g/mol |
| XLogP3 | 4.900 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 9 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 529.184 Da |
| 单同位素质量Monoisotopic Mass | 529.184 Da |
| 拓扑极表面积Topological Polar Surface Area | 97.600 Ų |
| 重原子数Heavy Atom Count | 39 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 817.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 象形图 | GHS07, GHS08, GHS09 |
|---|---|
| 信号词 | 危险 |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H360: 可能损害生育力或未出生的孩子 H361: 怀疑破坏生育力或未出生的孩子 H372: 通过长时间或反复暴露对器官造成损害 H373: 通过长时间或反复暴露对器官造成损害 H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响 H413: 可能对水生生物造成长期的有害影响 |
| 预防措施声明 |
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P264: 处理后要彻底洗手。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理(请参阅此标签上的...)。 P391: 收集溢出物 P302+P352: 如皮肤沾染:用水充分清洗。 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P203: 使用前,获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P318: 如果暴露或担心,请就医。 P337+P317: 如果眼睛刺激持续:寻求医疗帮助。 P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。 P319: 如果你感到不适,请寻求医疗帮助。 |
| 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 (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 (4874). [PMID:24786396] |
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