PQ401

SKU: orb1225776

Description

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.

Key Properties

• CAS Number: 196868-63-0
• MW: 341.79
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₆ClN₃O₂
• SMILES: O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=CC(Cl)=CC=C3OC
• Target: IGF-1R
• Solubility: DMSO: 32 mg/mL (93.62 mM)

Bioactivity

• In Vivo:
  PQ401 (50 or 100 mg/kg; i.p.; thrice a week) results in a significant dose-dependent reduction in tumor growth over the course of the study. PQ401 reduces the growth rate of MCNeuA cells implanted into mice. Animal model: Female mice were MCNeuA tumor cells. Dosage: 50 or 100 mg/kg. Administration: Administered i.p. thrice a week; 24 days. Result: Resulted in a significant dose-dependent reduction in tumor growth. Tumor growth in the animals treated with 100 mg/kg was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals.
• In Vitro:
  PQ401 (1, 5, 10, 25, and 50 μM; 3 days) inhibits proliferation of cultured MCF-7 cells grown in serum or IGF-I in MCF-7 cells. Twenty-four hours of treatment with 15 μM PQ401 induces caspase-mediated apoptosis. PQ401 inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1 μM. Cell Proliferation Assay Cell line: Breast cancer cells, MCF-7 cells. Concentration: 1, 5, 10, 25, and 50 μM. Incubation time: 3 days. Result: Significantly reduced proliferation (IC50, 8 μM) at concentrations in the range of 1 μM. Produced a dramatic reduction in cell number from pretreatment levels at concentrations >10 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PQ401 | PQ-401 | PQ 401

Quick Database Links

Gene Symbol

IGF-1R