Icotinib

SKU: orb1301029

Description

Icotinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 610798-31-7
• MW: 391.42
• Purity: 99.79%
• Formula: C₂₂H₂₁N₃O₄
• SMILES: C#Cc1cccc(Nc2ncnc3cc4OCCOCCOCCOc4cc23)c1
• Target: EGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:72 mg/mL (183.95 mM);Ethanol:6 mg/mL (15.33 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.11 mM)

Bioactivity

• Target IC50:
  EGFR:5 nM
• In Vivo:
  Icotinib shows an antitumor effect in different types of xenografts. Icotinib inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts at a dose of 120 mg/kg, respectively.
• In Vitro:
  Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR.
• Cell Research:
  Cells (103 /well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 °C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | 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

Conmana, BPI 2009, BPI2009, BPI-2009, BPI-2009H, EGFR, Icotinib

Compound Identifiers

PubChem CID

22024915