Copanlisib dihydrochloride

SKU: orb1308430

Description

Copanlisib dihydrochloride is a potent and selective pan-class I PI3K inhibitor with low nanomolar IC50 values. It demonstrates significant antitumor activity in preclinical models and exhibits high selectivity over other kinases. This compound is widely used in cancer research for investigating PI3K signaling in both cellular and animal studies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1402152-13-9
• MW: 553.44
• Purity: 99.16% (May vary between batches)
• Formula: C₂₃H₃₀Cl₂N₈O₄
• SMILES: Cl.Cl.COc1c(OCCCN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cnc(N)nc3)=Nc12
• Target: PI3K,Apoptosis,mTOR
• Solubility: H2O:125 mg/mL (225.86 mM);DMSO:1 mg/mL (1.81 mM)

Bioactivity

• Target IC50:
  PI3Kγ:6.4 nM|mTOR:45 nM|PI3Kβ:3.7 nM|PI3Kα:0.5 nM|PI3Kδ:0.7 nM
• In Vivo:
  In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (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, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition.
• In Vitro:
  In both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells.

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

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

Compound Identifiers

PubChem CID

135565785