RG13022

SKU: orb1304081

Description

RG13022

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 136831-48-6
• MW: 266.29
• Purity: 98.38%
• Formula: C₁₆H₁₄N₂O₂
• SMILES: COc1ccc(\C=C(\C#N)c2cccnc2)cc1OC
• Target: EGFR
• Solubility: DMSO:50 mg/mL (187.77 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.51 mM)

Bioactivity

• Target IC50:
  EGF:4 μM
• In Vivo:
  RG13022 suppresses tumor growth and extends the lifespan of tumor-bearing nude mice.
• In Vitro:
  RG13022 suppresses EGF-stimulated cancer cell proliferation and inhibits EGF receptor autophosphorylation in immunoprecipitates (IC50: 4 μM) in a cell-free reaction. It inhibits colony formation (IC50: 1 μM) and DNA synthesis (IC50: 3 μM) in HER 14 cells stimulated by 50 ng/mL EGF, dose-dependently. Additionally, RG13022 inhibits growth stimulated by insulin, insulin-like growth factor I, insulin-like growth factor II, or transforming growth factor alpha. It completely blocks estrogen-stimulated phosphorylation of the EGF receptor and estrogen-induced cell proliferation, indicating that functioning TK pathways are essential for estrogen action.
• Cell Research:
  40 mM stock solutions of RG13022 is made in 100% DMSO and diluted with the culture medium before addition to the cells. MH-85 cells and HER 14 cells are plated in culture medium in the presence or absence of increasing concentrations of RG-13022 or RG-14620 for 10 days. At the end of culture, the cells are fixed with 4% (v/v) formaldehyde and stained with hematoxylin. Numbers of colonies including more than 20 cells in each well are counted under the microscope.

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

HER1, EGFR, Epidermal growth factor receptor, ErbB-1, inhibit, Inhibitor, RG 13022, RG13022, RG-13022, Tyrphostin RG 13022, Tyrphostin RG13022, Tyrphostin RG-13022

Compound Identifiers

PubChem CID

5353927