Nilotinib(AMN-107)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Nilotinib是一种选择性的口服酪氨酸激酶抑制剂,作用于天然BCR-ABL (WT p210)以及突变BCR-ABL (E281K、E292K、F317L、M351T和F486S)的自磷酸化,IC50值分别为20、42、31、38、29 和41 nM [ 1 ] 。
Nilotinib基于imatinib的结构进行设计,并在新诊断的或imatinib抗药性的慢性髓细胞性白血病(CML)中显示出优势。在广泛范围的CML衍生和转染的细胞系中, Nilotinib对野生型BCR-ABL的效力比imatinib更强。Nilotinib在胃肠道基质肿瘤中同样有效。Nilotinib在KIT突变细胞中显示出抑制作用,包括KITV560del、KITK642E和KITV560G (IC50 值为108 nM)。Nilotinib对KIT双突变同样有效,例如KITV560del/V654A、KITV559D/D820Y、KITV560del/V654A (IC50:192 nM)和KITV559D/D820Y (IC50:297 nM)。此外,Nilotinib可以选择性地抑制PDGFRα和PDGFRβ。Nilotinib在FIP1L1-PDGFRα组成性活化的EOL-1细胞中抑制细胞增,IC50值为0.54 nM[ 1 ,2 ] 。
参考文献:
[1] Weisberg E, Manley P, Mestan J, et al. AMN107 (Nilotinib): a novel and selective inhibitor of BCR-ABL. British Journal of Cancer, 2006, 94(12): 1765-1769.
[2] Blay J Y, Von Mehren M. Nilotinib: a novel, selective tyrosine kinase inhibitor//Seminars in oncology. WB Saunders, 2011, 38: S3-S9.
- 1. Seung-Hwan Kwon, Sangjune Kim, et al. "A Novel, Selective c-Abl Inhibitor, Compound 5, Prevents Neurodegeneration in Parkinson's Disease." J Med Chem. 2021 Oct 28;64(20):15091-15110. PMID: 34583507
- 2.Saebom Lee ,Sangjune Kim ,et al."The c-Abl inhibitor, Radotinib HCl is neuroprotective in a preclinical Parkinson’s disease mouse model." Human Molecular Genetics, ddy143.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 529.53 |
Cas No. | 641571-10-0 |
Formula | C28H22F3N7O |
Synonyms | AMN-107; Tasigna; AMN107 |
Solubility | ≥26.5 mg/mL in DMSO; insoluble in H2O; ≥5 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)N3C=C(N=C3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验: [1] | |
细胞系 |
来自单个CML患者的CD34+细胞 |
制备方法 |
该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
5 μM,16 hours |
使用 |
Nilotinib培养16小时充分抑制CrkL磷酸化,但不诱导凋亡,总的CD34+细胞样品中仅表现出CrkL磷酸化的部分和可变抑制,抑制范围为49%至0%。 |
动物实验: [2] | |
动物模型 |
注射8093淋巴瘤细胞的C57Bl /6J小鼠 |
给药剂量 |
口服,75 mg/kg,每天 |
实验结果 |
载体处理的小鼠在移植后3周内濒临死亡,表现出明显的ALL症状。与对照组小鼠相比,Nilotinib治疗的小鼠存活时间显著延长。该结果清楚地表明,Nilotinib在体内非常有效地抑制白血病细胞的增殖。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1] J?rgensen H G, Allan E K, Jordanides N E, et al. Nilotinib exerts equipotent antiproliferative effects to imatinib and does not induce apoptosis in CD34+ CML cells. Blood, 2007, 109(9): 4016-4019. [2] Kaur P, Feldhahn N, Zhang B, et al. Nilotinib treatment in mouse models of P190 Bcr/Abl lymphoblastic leukemia. Mol Cancer, 2007, 6(10): 67-77. |
描述 | Nilotinib(AMN-107)是一种Bcr-Abl抑制剂,IC50小于30 nM。 | |||||
靶点 | Bcr-Abl | |||||
IC50 | 30 nM |
质量控制和MSDS
- 批次:
化学结构
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