Name: BAY 80-6946 (Copanlisib)
Price: 300.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Several phosphatidylinositol-3-kinase (PI3K) inhibitors are being investigated as a treatment for patients with B-cell malignancies. Such agents prevent activation of PI3K enzymes that are hyperactive in many B-cell malignancies and associated with tumor progression. Copanlisib is a novel pan-Class I phosphatidylinositol-3-kinase (PI3K) inhibitor with potent preclinical inhibitory activity against both PI3K-d and PI3K-α isoforms.In vitro: BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity, which inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines [1]. In vivo: BAY 80-6946 is generally well tolerated through the maximum tolerated dose (MTD) of 0.8 mg/kg. pharmacokinetics (PK) results support dosing weekly. Grade 2 or 3 hyperglycemia in the first 24 hrs after receiving a MTD dose. Pharmacokinetics, clinical SD as well as FDG-PET data are consistent with effective exposure and PI3K pathway inhibition. [2]. Clinical trial: Copanlisib (BAY 80-6946), developed by Bayer, is a selective Class I phosphoinositide 3-kinase inhibitor which has shown promise in Phase I/II clinical trials for the treatment of non-Hodgkin lymphoma and chronic lymphocytic leukemia. Phase II study shows that Copanlisib is active as a single-agent in heavily pretreated, advanced refractory/relapsed FL, MZL, , CLL and SLL. Copanlisib exhibited an acceptable toxicity profile, which was consistent with previous findings (https://ash.confex.com/ash/2014/webprogram/Paper70672.html).
    
    [1] Patnaik A, et al. J Clin Oncol, 29, 2011, (suppl, abstr 3035)
    [2] Andrea H, et al. Cancer Res, 2012; 72(8), (suppl, Abstract 869)
- Properties
  - Alternative Name
    
    2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
    
    CAS Number
    
    1032568-63-0
    
    Molecular Formula
    
    C23H28N8O4
    
    Molecular Weight
    
    480.52
    
    Appearance
    
    A solid
    
    Purity
    
    98.13%
    
    Solubility
    
    insoluble in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Almohazey D, Lo YH, et al. "The ErbB3 receptor tyrosine kinase negatively regulates Paneth cells by PI3K-dependent suppression of Atoh1." Cell Death Differ. 2017 May;24(5):855-865. PMID:28304405

BAY 80-6946 (Copanlisib)

BAY 80-6946 (Copanlisib)

Background

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