化合物AG-490 T2600

Product Introduction
Bioactivity


英文名: AG490

描述: AG490 (Tyrphostin B42) 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。

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)

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.

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。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 59 mg/mL (200.47 mM)
Ethanol : 6 mg/mL (20.38 mM)


关键字: Tyrphostin AG490 | Epidermal growth factor receptor | Inhibitor | Tyrphostin B-42 | ErbB-1 | STAT | Janus kinase | Autophagy | Tyrphostin B 42 | EGFR | HER1 | Tyrphostin AG-490 | inhibit | JAK | AG490

相关产品: (E)-AG 556 | ZM323881 hydrochloride | Rilzabrutinib | Nimotuzumab | Ginsenoside Rh2 | EGFR-IN-7 | Dacomitinib hydrate | Sunvozertinib | AZ-5104 | EGFR-IN-82

相关库: JAK-STAT Compound Library | Transcription Factor-Targeted Compound Library | Membrane Protein-targeted Compound Library | Human Metabolite Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Hematonosis Compound Library | Autophagy Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途