PQ401 hydrochloride (196868-63-0(free base))

SKU: orb1302951

Description

PQ401 is a potent small molecule inhibitor of IGF-1R autophosphorylation, exhibiting an IC50 of less than 1 µM. This compound is a valuable research tool for studying IGF-1R signaling in cancer biology and metabolic disorders, applicable in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• MW: 378.25
• Purity: 99.67% (May vary between batches)
• Formula: C₁₈H₁₇Cl₂N₃O₂
• SMILES: Cl.COc1ccc(Cl)cc1NC(=O)Nc1cc(C)nc2ccccc12
• Target: IGF-1R
• Solubility: DMSO:45 mg/mL (118.97 mM)

Bioactivity

• Target IC50:
  IGF-1R:<1 μM
• In Vivo:
  PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner.
• In Vitro:
  PQ 401 is an IGF-1R inhibitor and inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1 μM. PQ 401 significantly reduced proliferation of MCF-7 cells with IC50 of 8 μM. PQ 401 also inhibits growth of MCNeuA cells with IC50 of 15 μM. PQ 401 inhibits the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. PQ 401 increases caspase-mediated apoptotic activity in MCF-7 cells.
• Cell Research:
  Cell lines: MCF-7,MCNeuA. Concentrations: ~50 μM. Incubation Time: 3 days. Method: The inhibitory effects of diaryl urea on breast cancer cell growth are determined using a CyQuant cell proliferation assay kit.MCF-7 or MCNeuA cells are plated in 96-well plates (5×103 per well) in phenol red-free DMEM supplemented with 10% FCS.One plate isprepared for each harvest day.Cells are allowed to adhere overnight and are then treated with various concentrations of diaryl urea or DMSO as a vehicle control.Microplate cultures are harvested on days 0,1,2,and 3 by inverting the microplate onto paper towels with gentle blotting to remove growth medium without disrupting adherent cells.Each plate iskept at 80 ℃ until the end of the experiment (day 3) when all of the plates are thawed and assayed together.After thawing,200 μL of CyQuant GR solution are added to each well and the plates are incubated in the dark for 2 to 5 minutes.Fluorescence ismeasured with a SpectraMax Gemini XS fluorescence microplate reader with 480-nm excitation and 520-nm emission.Proliferation index iscalculated as the percent of nucleotide content versus control cells at day 0.
• Animal Research:
  Animal Models: FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells. Formulation: 8% polysorbate 80 and ethanol. Dosages: 50 or 100 mg/kg. Administration: i.p.

Storage & Handling

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

Alternative Names

PQ401 hydrochloride (196868 63 0(free base)), PQ401 hydrochloride (196868630(free base)), PQ-401 hydrochloride (196868-63-0(free base)), PQ401 hydrochloride (196868-63-0(free base)), IGF1R, IGF-1R

Compound Identifiers

PubChem CID

145875209