WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 204570
Description: Copanlisib, also known as BAY 80-6946, is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BAY 80-6946 inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.
MedKoo Cat#: 204570
Name: Copanlisib (BAY80-6946)
Chemical Formula: C23H28N8O4
Exact Mass: 480.22335
Molecular Weight: 480.52
Elemental Analysis: C, 57.49; H, 5.87; N, 23.32; O, 13.32
Synonym: BAY 80-6946; BAY80-6946; BAY806946; Copanlisib
IUPAC/Chemical Name: 2-amino-N-(7-methoxy-8-(3-morpholinopropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl)pyrimidine-5-carboxamide
InChi Key: PZBCKZWLPGJMAO-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H28N8O4/c1-33-19-17(35-10-2-6-30-8-11-34-12-9-30)4-3-16-18(19)28-23(31-7-5-25-20(16)31)29-21(32)15-13-26-22(24)27-14-15/h3-4,13-14H,2,5-12H2,1H3,(H2,24,26,27)(H,28,29,32)
SMILES Code: O=C(C1=CN=C(N)N=C1)NC2=NC3=C(C=CC(OCCCN4CCOCC4)=C3OC)C5=NCCN25.
BAY 80-6946 is a potent and highly selective reversible pan-Class I PI3K inhibitor with anti-tumor activity in a panel of preclinical models. A phase I dose escalation multicenter study showed that BAY 80-6946 was generally well tolerated through the MTD of 0.8 mg/kg. PK results support weekly dosing. Grade 2/3 hyperglycemia in the first 24 hrs after receiving a dose is common at the MTD. PK, clinical SD and FDG-PET data are consistent with effective exposure and PI3K pathway inhibition. (source: J Clin Oncol 29: 2011 (suppl; abstr 3035)
Tips for making stock solution
Due to its chemical nature, pure BAY80-6946 solid powder was found to have very low solubility in common organic solvents. This has been reported in the literature. User may use the following method as a reference when making stock solution: 2 mg BAY80-6946 is placed in a clear vial. To this vial, 10 ÂµL 10% HCl is added. The vial is capped and shaken for a few seconds to allow HCl solution to wet the crystals of BAY80-6946. Then 90 ÂµL water is added, and shaken for a few second, which will give a clear stock solution at 20 mg /mL. This solution can be further diluted using 0.5% HCl water solution.
This solution can be further diluted using 0.5% HCl water solution.
Pure BAY80-6946 has very low solubility, because of its chemical property, not because of the poor quality of our product. Molecule of BAY80-6946 contains several basic nitrogen atoms, after protonated by HCl, its solubility will be enhanced. For in vitro studies, 5 mmol/L stock solution of BAY 80-6946 (in dimethyl sulfoxide with 10 mmol/L trifluoroacetic acid) was used - see Mol Cancer Ther. 2013 Nov;12(11):2319-30.
1: Schneider P, SchÃ¶n M, Pletz N, Seitz CS, Liu N, Ziegelbauer K, Zachmann K, Emmert S, SchÃ¶n MP. The novel PI3 kinase inhibitor, BAY 80-6946, impairs melanoma growth in vivo and in vitro. Exp Dermatol. 2014 Jun 18. doi: 10.1111/exd.12470. [Epub ahead of print] PubMed PMID: 24942196.
2: Preliminary results of a phase II study of single agent Bay 80-6946, a Novel PI3K inhibitor, in patients with relapsed/refractory, indolent or aggressive lymphoma. Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):14-6. PubMed PMID: 24852792.
3: Liu N, Rowley BR, Bull CO, Schneider C, Haegebarth A, Schatz CA, Fracasso PR, Wilkie DP, Hentemann M, Wilhelm SM, Scott WJ, Mumberg D, Ziegelbauer K. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30. doi: 10.1158/1535-7163.MCT-12-0993-T. Epub 2013 Oct 29. PubMed PMID: 24170767.