化合物 AG-490|T2600|TargetMol

AG490
133550-30-8

￥188 5mg 起订

￥297 10mg 起订

￥563 25mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 AG-490

英文名称：: AG490

CAS号：: 133550-30-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.7%

产品类别：: 抑制剂

货号：: T2600

Product Introduction

Bioactivity

Name	AG490
Description	AG490 (Tyrphostin B42) 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.
Cell Research	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)
Kinase Assay	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.
In vitro	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.
In vivo	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。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 40 mg/mL (135.92 mM) Ethanol : 6 mg/mL (20.38 mM)
Keywords	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
Inhibitors Related	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Xylitol \| Hydroxychloroquine \| Curcumin \| Stavudine \| Myricetin \| Paeonol \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| JAK-STAT Compound Library \| Anti-Aging Compound Library \| Stem Cell Differentiation Compound Library \| Membrane Protein-targeted Compound Library \| Tyrosine Kinase Inhibitor Library

Zinc02557947|||Tyrphostin B42|||Tyrphostin AG 490|||AG-490|||AG 490|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子