Pelitinib

SKU: orb1305682

Description

Pelitinib

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 257933-82-7
• MW: 467.92
• Purity: 99.86%
• Formula: C₂₄H₂₃ClFN₅O₂
• SMILES: CCOc1cc2ncc(C#N)c(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C
• Target: Raf,MEK,EGFR,Src
• Solubility: DMSO:9.43 mg/mL (20.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.14 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  EGFR:38.5 nM
• In Vivo:
  Pelitinib (75-500 nM) specifically inhibits the activation of AKT and ERK1/2 without affecting the NF-κB pathway. In normal human keratinocytes, Pelitinib effectively inhibits TGF-α-mediated EGFR activation (IC50: 56 nM) and the activation of STAT3 and ERK1/2 (IC50: 60 nM and 62 nM, respectively). It also suppresses EGF-induced EGFR phosphorylation (IC50: 20-80 nM) and STAT3 phosphorylation (IC50: 30-70 nM) in both A431 cells and normal human keratinocytes. Moreover, Pelitinib significantly inhibits the proliferation of normal human keratinocytes (IC50: 61 nM), A431 (IC50: 125 nM), and MDA-468 (IC50: 260 nM) tumor cells, but shows lower activity against MCF-7 cells (IC50: 3.6 μM).
• In Vitro:
  In the A431 xenograft model targeting EGFR, Pelitinib (10 mg/kg, p.o.) effectively inhibits EGFR phosphorylation, achieving a 90% inhibition within 1 hour and maintaining over 50% inhibition after 24 hours. In the mouse airway epithelial cell remodeling model, which can be induced by viral infection and is characterized by a delayed yet permanent transition to goblet cell metaplasia, Pelitinib (20 mg/kg/day) completely blocks the increase of ciliated cells and the decrease of Clara cells, thereby correcting epithelial cell remodeling from three different aspects and significantly inhibiting the occurrence of goblet cells. Additionally, Pelitinib (20 mg/kg/day) inhibits 87% of tumor occurrence in APCMin/+ mice, which is comparable to the effect of a double dose of EKI-785 (40 mg/kg/day), consistent with its higher in vivo activity. Pelitinib exhibits selective inhibitory effects on EGFR signaling in airway epithelial cells in vivo.
• Cell Research:
  Cells are seeded in 96-well dishes, and after 2 hours, Pelitinib is added and incubated for 5 days. After incubation, the medium is removed from each well and fresh medium (150 μL) + 1 mg/mL MTT solution (50 μL) is added. After incubation for 2 hours at 37 °C, the medium is replaced with 150 μL DMSO, and absorbance at 540 nm in each well is determined. The IC50 is calculated by linear regression of the data. (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

Raf, WAY-EKB 569, WAY-EKB569, WAY-EKB-569, Pelitinib, Src, inhibit, EKB 569, EKB569, EKB-569, Epidermal growth factor receptor, EGFR, ErbB-1, Inhibitor, HER1, HER2/ErbB2, MEK

Compound Identifiers

PubChem CID

6445562