PD168393

SKU: orb1300334

Description

PD168393 is a potent and irreversible EGFR inhibitor (IC50: 0.70 nM) that selectively targets Cys-773. It demonstrates high selectivity, showing no activity against PKC, FGFR, PDGFR, or insulin receptor. This compound is widely used in vitro and in vivo to study EGFR-driven oncogenic signaling and tumor growth.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 194423-15-9
• MW: 369.22
• Purity: 99.13%
• Formula: C₁₇H₁₃BrN₄O
• SMILES: Brc1cccc(Nc2ncnc3ccc(NC(=O)C=C)cc23)c1
• Target: Autophagy,FGFR,PKC,EGFR,PDGFR,IGF-1R,Apoptosis
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.42 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:40 mg/mL (108.34 mM)

Bioactivity

• Target IC50:
  EGFR:0.70 nM
• In Vivo:
  PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration.
• In Vitro:
  PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb.

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

IGF1R, Inhibitor, Insulin Receptor, HER1, Epidermal growth factor receptor, epidermoid carcinoma, ErbB-1, EGFR, FGFR, inhibit, PDGFR, PD168393, PD-168393, PD 168393, Autophagy, Apoptosis, PKC, tumor

Compound Identifiers

PubChem CID

4708