计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
AG-1024 (Tyrphostin)能抑制IGF-1R自磷酸化，IC50为7 μM，而对IR的IC50则为57 μM。
Information
AG-1024 AG-1024 (Tyrphostin, AGS 200) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
In vitro
AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively. AG-1024 (10 μM) inhibits cell proliferation in a time-dependent manner, and induces apoptosis in MCF-7 cells at 48 hours by 20.1% and >40% when combined with irradiation (10 Gy), more potently than that of irradiation (10 Gy) alone by 11.8%, which is associated with a down-regulation of phospho-Akt1 and bcl-2, and up-regulation of Bax, p53 and p21. AG-1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes. AG-1024 treatment down-regulates the expression of Bcr-Abl and P-Akt, and up-regulates DNA-PKcs expression in UT7-9 and Ba/F3-p210 cells, leading to decreased clonogenic survival and proliferation. AG-1024 also significantly inhibits the proliferation of cells resistant to the BCR-ABL inhibitor STI571, which correlates with a dose-dependent decrease in Bcr-Abl protein expression.
In vivo
Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentration 10 μM
Incubation Time：24, 48 or 72 hours
Powder Purity:≥99%
规格
英文别名
Tyrphostin, AGS 200 | 2-(3-bromo-5-tert-butyl-4-hydroxybenzylidene)malononitrile
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AG-1024
生化机理
AG-1024（Tyrphostin，AGS 200）抑制 IGF-1R 自身磷酸化的 IC50 值为 7 μM，对 IR 的抑制作用较弱，IC50 值为 57 μM，并能特异性地区分 InsR 和 IGF-1R（与其他 tyrphostin 相比）。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
胰岛素样生长因子 I 受体抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O
分子量
305.17
Reaxy-Rn
2379618
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2379618&ln=
技术文档
高级数据
关联靶点（人）
IGF1R
Tclin
胰岛素类生长因子 1 受体(Insulin-like growth factor 1 receptor)
(1 活性数据)
CISD1
Tchem
CDGSH 铁硫结构域蛋白 1(CDGSH iron-sulfur domain-containing protein 1)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 G2409580 |
分析证书 | A408645 |
此产品的引用文献
溶液计算器
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