Copanlisib

SKU: orb1300871

Description

Copanlisib is a potent and selective PI3K inhibitor used in research to study tumor growth and survival mechanisms. It is applied in both in vitro and in vivo studies to investigate oncology, signal transduction, and resistance mechanisms in various cancers, including lymphomas.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1032568-63-0
• MW: 480.52
• Purity: 99.88% (May vary between batches)
• Formula: C₂₃H₂₈N₈O₄
• SMILES: O(C)C1=C2C(C=3N(C(NC(=O)C=4C=NC(N)=NC4)=N2)CCN3)=CC=C1OCCCN5CCOCC5
• Target: PI3K,Apoptosis
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);1M HCl:71.43 mg/mL (148.65 mM);0.01M HCl:10 mg/mL (20.81 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  PI3Kα:0.5 nM|PI3Kβ:3.7 nM|PI3Kγ:6.4 nM|mTOR:45 nM|PI3Kδ:0.7 nM
• In Vivo:
  In rat KPL4 or HCT116 tumor xenograft model, Copanlisib (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, Copanlisib (14 mg/kg, i.v.) also causes tumor growth inhibition.
• In Vitro:
  In both KPL4 cells and LPA-stimulated PC3 cells, Copanlisib reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, Copanlisib shows antiproliferative activity and induces apoptosis. The combination of HER2-targeted therapies and Copanlisib inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells.
• Cell Research:
  Cell proliferation over a 72-hour period is determined using the CellTiter-Glo luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37oC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37oC. Luminescence values are determined with a Wallac 1420 Victor2 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.(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

inhibit, intravenous, Inhibitor, Apoptosis, antitumor, antiproliferative, BAY 80-6946, administration, AKT, Copanlisib, sub-nanomolar, Phosphoinositide 3-kinase, PI3Kγ, PI3Kδ, PI3Kβ, PI3Kα, phosphorylation, PI3K

Compound Identifiers

PubChem CID

135565596