Tyrphostin AG 879

SKU: orb1300532

Description

Tyrphostin AG 879 is a selective inhibitor of the HER2/ErbB2 tyrosine kinase, demonstrating potent activity with an IC50 of 1 μM. It exhibits 100- to 500-fold selectivity for HER2 over EGFR and PDGFR, making it a valuable tool for investigating HER2-driven signaling in cancer research, both in cellular and animal models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 148741-30-4
• MW: 316.46
• Purity: 99.05% (May vary between batches)
• Formula: C₁₈H₂₄N₂OS
• SMILES: CC(C)(C)c1cc(\C=C(/C#N)C(N)=S)cc(c1O)C(C)(C)C
• Target: Apoptosis,Trk receptor,HER,PDGFR,EGFR
• Solubility: DMSO:31.7 mg/mL (100.17 mM);Ethanol:7.9 mg/mL (24.96 mM)

Bioactivity

• Target IC50:
  HER2/ErbB2:1 μM
• In Vivo:
  AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells.
• In Vitro:
  AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937).
• Cell Research:
  Cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.(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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ErbB-1, ErbB2, EGFR, Epidermal growth factor receptor, HER2-Neu, HER1, Inhibitor, p75, inhibit, Apoptosis, Antitumor, antiproliferation, AG879, AG-879, AG 879, PDGFR, phosphorylation, Tyrphostin AG 879, Tyrphostin AG879, Tyrphostin AG-879, tyrosine, Tropomyosin related kinase receptor, Trkreceptor, Trk, Trk receptor, Trk Receptor, TrKA

Compound Identifiers

PubChem CID

135419190