AG-1024
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AG1024是胰岛素样生长因子-1受体(IGF-1R)和胰岛素受体(IR)的抑制剂,特异性抑制IGF-1R和IR自磷酸化,IC50值分别为7 μM和57 μM[1]。
实验表明,AG1024抑制NIH-3T3小鼠成纤维细胞中IGF-1和胰岛素刺激的细胞增殖,IC50值分别为0.4 μM和0.1 μM。此外,AG1024也抑制酪氨酸激酶作用于外源底物(TKA)的活性,IC50值分别为18 μM和80 μM[1]。
据报道,AG1024阻断受体酪氨酸激酶活性,以致阻断MAPK和Akt信号通路,抑制细胞生长。此外,研究表明,AG1024浓度依赖性地抑制MCF-7:PF细胞中的E2刺激[2]。
参考文献:
[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr; 138(4):1427-33.
[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2. Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 305.17 |
Cas No. | 65678-07-1 |
Formula | C14H13BrN2O |
Solubility | insoluble in H2O; ≥11.23 mg/mL in EtOH; ≥15.25 mg/mL in DMSO |
Chemical Name | 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O |
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 |
MCF-7 |
溶解方法 |
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 |
10 nM,抑制细胞增殖的时间为5天,诱导凋亡的时间为48小时 |
实验结果 |
酪氨酸磷酸化抑制剂AG1024以时间依赖性方式显著降低细胞增殖,它还有效地诱导细胞凋亡,凋亡细胞占20.1%。 |
动物实验[2]: | |
动物模型 |
植入Baf3-p210细胞的雌性裸鼠 |
剂量 |
腹腔注射,30 μg溶于100 μl,每天一次,为期10天 |
实验结果 |
在注射表达Bcr-Abl的Ba/F3-p210细胞后,使用PBS 0.1 ml注射裸鼠6天作为对照组,使用酪氨酸磷酸化抑制剂AG1024 30 μg/100 μl注射裸鼠作为实验组,1 μl含有980 μM酪氨酸磷酸化抑制剂AG1024。当用酪氨酸磷酸化抑制剂AG1024处理小鼠时,Ba/F3-p210异种移植物的生长显著延迟。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Wen B, Deutsch E, Marangoni E, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. British journal of cancer, 2001, 85(12): 2017. [2] Deutsch E, Maggiorella L, Wen B, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. British journal of cancer, 2004, 91(9): 1735-1741. |
描述 | AG-1024是IGF-1R的选择性抑制剂,其IC50值为7 μM。 | |||||
靶点 | IGF-1R | |||||
IC50 | 7 μM |