PD176252

SKU: orb1706834

Description

PD176252 is a dual bombesin receptor (BB1/BB2) antagonist and a formyl peptide receptor (FPR1/FPR2) agonist. This small molecule inhibitor suppresses cancer cell growth and proliferation, making it a valuable tool for oncology research in both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 204067-01-6
• MW: 584.67
• Purity: 99.18% (May vary between batches)
• Formula: C₃₂H₃₆N₆O₅
• SMILES: COc1ccc(nc1)C1(CNC(=O)[C@](C)(Cc2c[nH]c3ccccc23)NC(=O)Nc2ccc(cc2)[N+]([O-])=O)CCCCC1
• Target: Bombesin Receptor
• Solubility: DMSO:100 mg/mL (171.04 mM);10% DMSO+90% Corn Oil:5 mg/mL (8.55 mM)

Bioactivity

• Target IC50:
  FPR1:0.31 μM (EC50)|BB1 receptor:0.66 nM (Ki, Rat)|BB1 receptor:0.17 nM (Ki, Human)|FPR:0.72±0.21 μM (EC50, human)|BB2 receptor:16 nM (Rat)|BB2 receptor:1 nM (Ki, Human)|FPR2:0.66 μM (EC50)
• In Vivo:
  Orally administered PD176252 (1, 10 μg) potently inhibits the growth and proliferation of NCI-H1299 xenografts in nude mice.
• In Vitro:
  PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptors, with Kis of 0.17 nM and 1 nM for human BB1 and BB2, and 0.66 nM and 16 nM for rat BB1 and BB2 receptors, respectively. In CHO cells expressing human BB1 or BB2 receptors, PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C with appKBs of 4.0 nM and 13 nM, respectively. It also blocks bombesin-evoked increases in intracellular calcium levels, with appKBs of 2.3 nM and 36 nM, respectively. Additionally, PD176252 is an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells, activating Ca2+ mobilization in HL-60 cells transfected with human FPRs (EC50, 0.72 ± 0.21 μM). PD176252 shows little specific 125I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM but suppresses almost all specific binding at 1000 nM, with an IC50 of 30 nM. Furthermore, PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC50s of 7 and 5 μM.

Storage & Handling

• Storage: store under nitrogen | 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

BB1, BB2, BombesinReceptor, Bombesin Receptor, PD176252, PD-176252, PD 176252, Human BB1 receptor, Human BB2 receptor, FPR2, FPR1, Rat BB1 receptor, Rat BB2 receptor

Compound Identifiers

PubChem CID

9829828