Copanlisib

SKU: orb1300871

Description

Copanlisib

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1032568-63-0
• MW: 480.52
• Purity: 99.05%
• Formula: C₂₃H₂₈N₈O₄
• SMILES: O(C)C1=C2C(C=3N(C(NC(=O)C=4C=NC(N)=NC4)=N2)CCN3)=CC=C1OCCCN5CCOCC5
• Target: Apoptosis,PI3K
• 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