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 2 篇同行评审文献引用。
概述
AG-490 (Tyrphostin AG 490)是EGFR抑制剂，IC50为100nM，比对ErbB2的抑制性高135倍，对Lck，Lyn，Btk，Syk和Src无活性。Tyrphostin AG has been used to block IL-6 cytokine signaling to study its effects on glial cell reactivity. AG 490 has also been used as a JAK2 inhibitor in human umbilical vein endothelial cells
Information
AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor ofEGFRwithIC50of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibitsJAK2with no activity to Lck, Lyn, Btk, Syk and Src.
In vitro
AG-490 inhibits HER-2 driven cell proliferation with IC50 of 3.5 μM. Corresponding to the specific dose-dependent inhibition of constitutively activated JAK2 in pre-B acute leukemia (ALL) cells, AG-490 (5 μM) almost completely blocks the growth of all ALL cells by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 does not inhibit the activities of Lck, Lyn, Btk, Syk, and Src. AG-490 (60-100 μM) blocks the constitutive activation of Stat3sm, and inhibits spontaneous as well as interleukin 2-induced growth of mycosis fungoides (MF) tumor cells with IC50 values of 75 μM and 20 μM, respectively. AG-490 potently inhibits IL-2-mediated human T cell growth with an IC50 of 25 μM by blocking the activities of JAK3 and STAT5a/b. Although AG-490 alone has no effect on proliferation of FDrv210H cells at a concentration of 5 μM, AG-490 can synergize with STI571 to enhance its inhibitory effect on p210bcr-abl driven proliferation. AG-490 significantly inhibits the constitutive activation of Stat3 in MOPC, MPC11, and S194 cells, leading to dramatic dose-dependent apoptosis. AG-490 (100 μM) inhibits Akt phosphorylation, inhibits the activation of nuclear factor-κB, and causes the activation of GSK-3β, leading to the reduction of c-Myc. AG-490 (50 μM) can induce apoptosis of imatinib-resistant BaF3 cells expressing T315I and E255K mutants of Bcr-Abl. AG-490 at 30 μM inhibits not only Epo-induced phosphorylation of wild-type JAK2 but also constitutive phosphorylation of the JAK2 V617F mutant. AG-490 also potently inhibits cytokine-independent cell growth induced by the JAK2 V617F mutant in BaF3 cells.
In vivo
Administration of AG-490 drastically reduces the numbers of CD45+ and HLA-DR+ cells from 48 % and 46% in bone marrow of untreated mice, as well as 38% and 22% in the spleen of untreated mice to undetectale levels. In vivo administration of AG-490 causes murine myeloma tumor cell apoptosis but does not inhibit IL-12-mediated macrophage activation and IFN-γ production by lymphocytes. Consistent with the in vitro blocking of JAK2 V617F mutant activity, AG-490 treatment at 0.5 mg/day for 10 days effectively inhibits JAK2 V617F mutant-induced tumorigenesis and tumor cell invasion in nude mice. Combined therapy with AG-490 and IL-12 induces greater antitumor effects than either agent alone in a murine myeloma tumor model.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~ 50 μM
Incubation Time：16 hours
Powder Purity:≥99%
规格
英文别名
Zinc02557947 | (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AG-490 (Tyrphostin B42)
生化机理
AG-490 （Tyrphostin B42，Zinc02557947）是表皮生长因子受体（EGFR）的抑制剂，在无细胞实验中的 IC50 为 0.1 μM，对 EGFR 的选择性比 ErbB2 高 135 倍，还能抑制 JAK2，但对 Lck、Lyn、Btk、Syk 和 Src 没有活性。
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
表皮生长因子受体抑制剂
名称和识别符
EC号
664-282-2
分子类型
小分子
Isomeric SMILES
C1=CC=C(C=C1)CNC(=O)/C(=C/C2=CC(=C(C=C2)O)O)/C#N
分子量
294.3
Reaxy-Rn
8338789
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8338789&ln=
技术文档
高级数据
关联靶点（人）
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 44 mg/mL (196.16 mM); Ethanol: -1 mg/mL
熔点
215°C
安全和危险性（GHS）
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 |
|---|---|---|
 J2429003 |
分析证书 | A408508 |
技术文档和文章
此产品的引用文献
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
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