AG490

SKU: orb1305279

Description

AG490

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 133550-30-8
• MW: 294.3
• Purity: 99.85%
• Formula: C₁₇H₁₄N₂O₃
• SMILES: C(=C(/C(NCC1=CC=CC=C1)=O)\C#N)\C2=CC(O)=C(O)C=C2
• Target: JAK,EGFR,Autophagy,STAT
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (16.99 mM);DMSO:245 mg/mL (832.48 mM);Ethanol:6 mg/mL (20.39 mM)

Bioactivity

• Target IC50:
  EGFR:0.1 μM
• In Vivo:
  AG-490 induces programmed cell death, almost completely inhibitin 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 an 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 inhibit 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 FDrv21 h cell proliferation alone at 5 μM, it enhance the inhibitory effect of STI571 on p210bcr-abl, thus promoting ant Proliferative activity.
• In Vitro:
  in vivo treatment with AG-490 facilitates apoptosis in mouse myeloma cells without impairin the activation of macrophages o 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 b the JAK2 V617F mutation. Additionally, AG-490 markedly reduce 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.
• Cell Research:
  Cells are exposed to different concentration of AG-490 for 16 hours. Fo the determination of cell proliferation, [3H]tymidine (1 μCi) is added 6 hours or more befor the cultures are terminated. Cells are then collected and Samples counted in a liquid scintillation counter. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

HER2/ErbB2, EGFR, JAK, JAK2, AG 490, AG490, AG-490, Autophagy, Zinc02557947, STAT, Tyrphostin B 42, Tyrphostin B42, Tyrphostin B-42, Tyrphostin AG490, Tyrphostin AG-490, Tyrphostin AG 490

Compound Identifiers

PubChem CID

5328779