AG 1295

SKU: orb1308685

Description

AG 1295 is a potent and selective small molecule inhibitor of the platelet-derived growth factor receptor (PDGFR) tyrosine kinase. It specifically blocks PDGFR autophosphorylation while sparing the EGF receptor, making it a valuable tool for studying PDGF signaling in cancer research and cellular proliferation assays both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 71897-07-9
• MW: 234.3
• Purity: 99.64%
• Formula: C₁₆H₁₄N₂
• SMILES: Cc1cc2ncc(nc2cc1C)-c1ccccc1
• Target: PDGFR
• Solubility: DMSO:60 mg/mL (256.08 mM)

Bioactivity

• In Vivo:
  AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibiting PDGFR-beta-triggered tyrosine phosphorylation. AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly decreases interstitial fibrosis, as evidenced by a smaller Sirius-Red stained area, fewer macrophages, reduced ED-A+ fibronectin deposition, and fewer alpha-smooth muscle actin-positive cells.
• In Vitro:
  AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro. AG 1295 inhibits PDGFR autophosphorylation with IC50s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively.

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

Inhibitor, inhibit, Platelet-derived growth factor receptor, PDGFR, autophosphorylation, AG1295, AG-1295, AG 1295, RTK, PDGF-receptor

Compound Identifiers

PubChem CID

2048