AG-490

SKU: orb1305279

Description

AG490

Research Area

Cell Biology

Key Properties

• CAS Number: 133550-30-8
• MW: 294.3
• Purity: >98%
• Formula: C₁₇H₁₄N₂O₃
• SMILES: C(=C(/C(NCC1=CC=CC=C1)=O)\C#N)\C2=CC(O)=C(O)C=C2
• Target: Kinase
• Solubility: Soluble in DMSO (up to 25 mg/ml), in DMF (up to 40 mg/ml) or in Ethanol (up to 10 mg/ml).

Bioactivity

• Target IC50:
  EGFR:0.1 μM
• In Vivo:
  AG-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.
• In Vitro:
  In 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.
• 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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• 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