AG-1478

SKU: orb1306646

Description

AG-1478 (Tyrphostin AG-1478, NSC-693255) is a potent and selective inhibitor of the Epidermal Growth Factor Receptor (EGFR). It is widely used in biochemical and cell-based research to study EGFR-driven signaling pathways, proliferation, and tumorigenesis in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Infectious Disease & Virology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 153436-53-4
• MW: 315.75
• Purity: 99.71% (May vary between batches)
• Formula: C₁₆H₁₄ClN₃O₂
• SMILES: N(C=1C2=C(C=C(OC)C(OC)=C2)N=CN1)C3=CC(Cl)=CC=C3
• Target: PDGFR,Influenza Virus,HCV Protease,EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.17 mM);DMSO:10 mg/mL (31.67 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR:3 nM
• In Vivo:
  At a concentration of 0.25 μM, AG-1478 effectively inhibits Ang II, Ca2+ ionophore, and EGF-induced MAPK activation in VSMCs, without affecting fosinopril or platelet-derived growth factor-BB (PDGF-BB)-induced MAPK activation. AG-1478 also suppresses EGF-induced mitosis in BaF/ERX and LIM1215 cells, with IC50 values of 0.07 μM and 0.2 μM, respectively. Furthermore, AG-1478 inhibits the function of ABC (ATP-binding cassette) transport proteins, such as ABCB1 and ABCG2, showing a more significant effect on ABCG2. In comparison to cells expressing endogenous wild-type EGFR or overexpressing exogenous wild-type EGFR (with IC50 values of 34.6 μM and 48.4 μM respectively), AG-1478 preferentially inhibits U87 mg cells expressing ΔEGFR, with an IC50 of 8.7 μM. It also preferentially inhibits tyrosine kinase activity and autophosphorylation of ΔEGFR over endogenous or overexpressed exogenous wild-type EGFR.
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• In Vitro:
  Co-administration of 0.4 mg AG-1478 with a single dose of 25 μCi 90Y-CHX-A''-DTPA-hu3S193 results in significantly enhanced potency compared to the drugs administered separately. AG-1478 blocks phosphorylation of EGFR at tumor sites and inhibits growth in xenograft models of A431 cells overexpressing wt EGFR and glioma expressing de2-7 EGFR. Even subtherapeutic doses of AG-1478 significantly increase the potency of cytotoxic drugs. The combination of AG-1478 and temozolomide shows synergistic antitumor activity against human glioma xenografts.
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• Cell Research:
  Cells are exposed to different concentrations of AG-1478 for 72 hours in 96-well plates. The effects of AG-1478 on cell growth are examined using an Alamar Blue assay. A 20-μL aliquot of Alamar Blue is added to each well, and its absorbance is determined using a Spectromax Scanning Micro plate Reader. The effects of AG-1478 are expressed as percentage of growth inhibition using untreated cells as the control (0% inhibition). Cellular DNA synthesis is determined using a [3H]thymidine incorporation assay. (Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PDGFR, virus, Tyrphostin AG1478, Tyrphostin AG-1478, Tyrphostin AG 1478, HCV, HCVProtease, HCV Protease, Hepatitis C virus, HER1, HER2, Inhibitor, injury, EGFR, encephalomyocarditis, EMCV, Epidermal growth factor receptor, ErbB-1, inhibit, NSC 693255, InfluenzaVirus, Influenza Virus, myocardial, NSC693255, NSC-693255, obesity, cancer, cardiovascular, antiviral, AG1478, AG-1478, AG 1478, chemotherapy, diseases

Compound Identifiers

PubChem CID

2051