| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
AG490 是一种 EGFR 抑制剂 ,IC50为 0.1 μM。它对 EGFR 的选择性比 ErbB2 高 135 倍,还抑制 JAK2。
产品描述 | AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src. |
靶点活性 | EGFR:0.1 μM |
体外活性 | 在体内,AG-490处理可促使小鼠骨髓瘤细胞凋亡,但不影响IL-12诱导的巨噬细胞活化和IFN-γ产量.AG-490(0.5 mg/day)处理裸鼠10天,对JAK2 V617F突变诱导的肿瘤形成及入侵有显著抑制效果.AG-490可大幅降低CD45+和HLA-DR+细胞数,在骨髓中,其可使上述细胞数分别从48% 和46%降低到不可检测水平,这未处理小鼠脾脏中,则从38%和 22% 降低到不可检测水平. |
体内活性 | 通过诱导程序性细胞死亡,AG-490(5 μM)几乎完全抑制所有ALL 细胞生长,而不影响正常造血功能。AG-490(30 μM)既对Epo诱导的野生型JAK2磷酸化有抑制作用,也对组成型的JAK2 V617F突变型磷酸化有抑制作用。AG-490(50 μM)对表达Bcr-Abl 突变型E255K和T315I的抗Imatinib的BaF3细胞凋亡具有诱导作用。AG-490(60-100 μM)对Stat3sm组成型激活有抑制作用,且抑制自发的(IC50:75 μM)或IL-2诱导的(IC50:20 μM)蕈菌肿瘤细胞生长。AG-490(100 μM)抑制Akt磷酸化和核因子-κB激活,且激活GSK-3β并导致c-Myc降低。AG-490对EGF依赖的HER 14细胞增殖有抑制作用(IC50:3.5 μM)。通过对JAK3和 STAT5a/b活性的抑制,AG-490有效抑制IL-2调节的人T细胞生长(IC50:25 μM)。 尽管AG-490 (5 μM)单独给药不影响FDrv210H细胞增殖,但其可协同增强STI571对p210bcr-abl的抑制从而促进增殖效果。 |
激酶实验 | In vitro kinase autophosphorylation: AG-490 is dissolved in DMSO 10%-Water-ethanol 45%. Crude membrane extracts (0.125 μg/mL) are preactivated with EGF (20 nM) in 50 mM HEPES buffer, pH 7.6, and 125 mM NaCl, for 15 minutes at 4 °C. Autophosphorylation activity of EGFR or ErbB2 kinase is assayed at 4 °C for 30 seconds in V-shaped 96-well plates. Membrane extracts (8 μL) are added to each well containing reaction mixture (12 μL, 50 mM, HEPES, pH 7.4,125 mM NaCl, 12 mM M8Ac2, 2 mM MnCl2, 1 mM NaVO3, 1 μM ATP, and 1 μCi[γ-32P]ATP, final concentrations) and increasing concentrations of AG-490 (4 μL). After termination by addition of hot sample buffer, the samples are run on a 6% SDS-polyacrylamide gel electrophoresis minigel, the gels dried, and autoradiography performed during the linear exposure time period. The receptor bands are scanned densitrometrically, and the results analyzed by the Ez-Fit program. For the analysis of autophosphorylation of JAK2, JAK2 is immunoprecipitated by using anti-JAK2 antibody from lysates of G2 cells pretreated for 16 hours with increasing concentrations of AG-490 (0-50 μM). Immune complexes are then immunoblotted with anti-phosphotyrosine antibody. A dose-dependent inhibition of in vitro kinase activity is demonstrated by assessing JAK2 autophosphorylation. |
细胞实验 | Cells are exposed to different concentrations of AG-490 for 16 hours. For the determination of cell proliferation, [3H]tymidine (1 μCi) is added 6 hours or more before the cultures are terminated. Cells are then collected and samples counted in a liquid scintillation counter. (Only for Reference) |
别名 | AG 490, Tyrphostin B42, AG-490, Zinc02557947, Tyrphostin AG 490 |
分子量 | 294.3 |
分子式 | C17H14N2O3 |
CAS No. | 133550-30-8 |
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 59 mg/mL (200.47 mM)
Ethanol: 6 mg/mL (20.38 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AG490 133550-30-8 Angiogenesis Autophagy Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors EGFR STAT JAK Epidermal growth factor receptor Inhibitor Tyrphostin AG490 Tyrphostin B-42 ErbB-1 AG 490 Janus kinase Tyrphostin B42 AG-490 Zinc02557947 Tyrphostin B 42 HER1 inhibit Tyrphostin AG 490 Tyrphostin AG-490 inhibitor