Tyrphostin 23

SKU: orb1306589

Description

Tyrphostin 23

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 118409-57-7
• MW: 186.17
• Purity: 99.19%
• Formula: C₁₀H₆N₂O₂
• SMILES: Oc1ccc(C=C(C#N)C#N)cc1O
• Target: EGFR
• Solubility: DMSO:35 mg/mL (188 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:35 mg/mL (188 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (10.74 mM)

Bioactivity

• Target IC50:
  EGFR:11 μM (Ki)|EGFR:35 μM
• In Vivo:
  AG18 inhibits the volume-sensitive release of [3H] taurine in primary astrocyte cultures in a dose-dependent manner. Additionally, AG18 suppresses EGF-induced autophosphorylation of EGFR in A431 cells with an IC50 value of 15 μM and inhibits the proliferation of GH3 cells induced by EGF at a concentration of 10 μM. At the same concentration, AG18 also prevents the increase in ERK1/2 phosphorylation stimulated by Ghrelin in GH3 cells and counteracts 2xKCl-induced contractions, exerting maximal inhibitory effects. At 100 μM, AG18 blocks the activity of IKK stimulated by TNF-alpha and TPA in A549 epithelial cells. Furthermore, at a concentration of 300 μM, it dose-dependently inhibits the stimulation of ICAM-1 expression induced by TPA in A549 epithelial cells. Additionally, at this concentration, AG18 also hampers the TPA-stimulated NF-kappaB DNA-binding and ICAM-1 promoter activity in A549 epithelial cells.
• Cell Research:
  GH3 cells are plated at 5 × 104 cells/well in media containing 2% charcoal-stripped FCS and various concentrations of ghrelin, desoctanoylated ghrelin and PMA or EGF for 72 hours with the addition of 2 μCi/well [3H]thymidine for a further 6 hours. A time-course of 24 hours, 48 hours and 72 hours is performed for ghrelin stimulation and 72 hours is selected for further experiments. Studies are also performed to investigate the effect of rat ghrelin or desoctanoyl ghrelin-induced proliferation and the effect of U0126, GF109203X, AG 18, wortmannin and H-89 upon ghrelin-induced MAPK stimulation. AG 18 at 10 μM is added 30 min before each treatment. Cells are harvested before counting in the presence of scintillation fluid using a Microbeta 1450 bcounter. Experiments are repeated at least three times.(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

RG 50810, RG50810, RG-50810, Tyrphostin 23, Tyrphostin A 23, Tyrphostin A23, Tyrphostin A-23, Tyrphostin23, Tyrphostin-23, TX 825, TX825, TX-825, AG18, AG-18, AG 18, inhibit, HER1, Inhibitor, ErbB-1, Epidermal growth factor receptor, EGFR

Compound Identifiers

PubChem CID

2052