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Postion:Product Catalog >Biochemical Engineering>Amino Acids and Derivatives>Tyrosine derivatives>AG490
AG490
  • AG490

AG490 NEW

Price $43 $64 $79
Package 10mg 25mg 50mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: AG490 CAS No.: 133550-30-8
Purity: 99.7% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameAG490
DescriptionAG490 (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 ResearchCells 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 AssayIn 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 vitroIn vivo, treatment with AG-490 facilitates apoptosis in mouse myeloma cells without impairing the activation of macrophages or the production of IFN-γ induced by IL-12. When administered at 0.5 mg/day for 10 days to nude mice, AG-490 significantly impedes tumor formation and invasion driven by the JAK2 V617F mutation. Additionally, AG-490 markedly reduces the numbers of CD45+ and HLA-DR+ cells; in the bone marrow, it diminishes their levels from 48% and 46% to undetectable, respectively, and in untreated mouse spleens, from 38% and 22% to undetectable levels.
In vivoAG-490 induces programmed cell death, almost completely inhibiting the growth of all ALL cells at 5 μM, without affecting normal hematopoietic functions. At 30 μM, it inhibits phosphorylation in both Epo-induced wild-type JAK2 and the constitutively active JAK2 V617F mutant. AG-490 at 50 μM induces apoptosis in Imatinib-resistant BaF3 cells expressing Bcr-Abl mutations E255K and T315I. Additionally, at 60-100 μM, it suppresses constitutive activation of Stat3sm and inhibits spontaneous (IC50: 75 μM) or IL-2 induced (IC50: 20 μM) mycelial tumor cell growth. At 100 μM, AG-490 inhibits Akt phosphorylation and NF-κB activation, activates GSK-3β, and results in a reduction of c-Myc. It also inhibits the proliferation of EGF-dependent HER 14 cells (IC50: 3.5 μM) by blocking JAK3 and STAT5a/b activities, effectively suppressing IL-2 regulated human T cell growth (IC50: 25 μM). While AG-490 does not affect FDrv210H cell proliferation alone at 5 μM, it enhances the inhibitory effect of STI571 on p210bcr-abl, thus promoting antiproliferative activity.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 40 mg/mL (135.92 mM)
Ethanol : 6 mg/mL (20.38 mM)
KeywordsTyrphostin 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 RelatedStavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib
Related Compound LibrariesReprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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