PD168393

SKU: orb1223205

Description

PD-168393 is a potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 700 pM).

Key Properties

• CAS Number: 194423-15-9
• MW: 369.22
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₃BrN₄O
• SMILES: C=CC(=O)Nc1cc2c(cc1)ncnc2Nc1cc(ccc1)Br
• Target: GluR
• Solubility: DMSO : ≥ 30 mg/mL. 81.25 mM

Bioactivity

• In Vivo:
  PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective In vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice. Animal model: A431 human epidermoid carcinoma grown as a xenograft in nude mice. Dosage: 58 mg/kg. Administration: Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28. Result: Suppressed the growth of human epidermoid carcinoma xenografts.
• In Vitro:
  PD168393 inhibits ligand-dependent receptor phosphorylation and inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 values of 4.3 nM and 5.7 nM, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PD168393 | PD 168393 | PD-168393

Quick Database Links

Gene Symbol

GluR