PD153035 hydrochloride

SKU: orb1307512

Description

PD153035 hydrochloride is a potent and highly selective EGFR inhibitor with a Ki of 5.2 pM, demonstrating minimal activity against FGFR, PDGFR, and other kinases. It is widely used in cancer research to study EGFR-driven signaling pathways in both cellular and animal models of tumorigenesis.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 183322-45-4
• MW: 396.67
• Purity: >99.99% (May vary between batches)
• Formula: C₁₆H₁₅BrClN₃O₂
• SMILES: Cl.COc1cc2ncnc(Nc3cccc(Br)c3)c2cc1OC
• Target: EGFR
• Solubility: DMSO:4 mg/mL (10.08 mM)

Bioactivity

• Target IC50:
  EGFR:5.2 pM(Ki)
• In Vivo:
  PD153035 exhibits dose-dependent inhibition of nasopharyngeal carcinoma cell lines HONE1 (IC50: 18.6 μM), NPC-TW04 (IC50: 9.8 μM), and NPC-TW01 (IC50: 12.9 μM). It also inhibits the epidermal growth factor receptor (EGFR) tyrosine kinase related to A-431 human squamous epithelial carcinoma (Ki: 5.2 pM, IC50: 29 pM). In Caco-2 colon cancer cells, PD153035 silences COX-2 expression induced by the PAR(2) activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI). Furthermore, PD153035 selectively inhibits EGF-induced tyrosine phosphorylation in Swiss 3T3 fibroblasts and A-431 human squamous epithelial cancer cells (IC50: 15 nM and 14 nM, respectively). When acting on human cancer cell lines overexpressing the EGF receptor, PD153035 suppresses cell growth, including in A431, DU145, Difi, ME180, and MDA-MB-468, with IC50 values of 0.22 μM, 0.4 μM, 0.3 μM, 0.95 μM, and 0.68 μM, respectively.
• In Vitro:
  When administered to HFD-fed mice, PD153035 enhances glucose tolerance, insulin sensitivity, and signaling while reducing subclinical inflammation. In immunodeficient nude mice carrying A431 human epidermoid carcinoma xenografts, PD153035 (80 mg/kg) inhibits the tyrosine kinase activity of the EGF receptor.
• Cell Research:
  Cells are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.(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

SU 5271, SU5271, SU-5271 Hcl, SU-5271, ZM252868, ZM-252868, ZM 252868 HCl, Tyrphostin AG 1517, Tyrphostin AG1517, Tyrphostin AG-1517, EGFR, PD 153035 Hydrochloride, PD 153035, PD-153035, PD153035 HCl, PD153035, AG 1517 Hcl, AG 1517, AG-1517, AG1517

Compound Identifiers

PubChem CID

11246488