BAY80-6946
BAY80-6946 is an inhibitor of p110α PI3K that exhibits anticancer chemotherapeutic activity. BAY80-6946 is currently in clinical trials and shows some benefit in the treatment of pancreatic cancer. In cellular and animal models of multiple myeloma, BAY80-6946 inhibits cell cycle progression, induces apoptosis, and inhibits cell proliferation and tumor growth.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18843052
| Cas No. |
1032568-63-0 |
|---|---|
| Purity |
≥98% |
| Formula |
C23H28N8O4 |
| Formula Wt. |
480.52 |
| IUPAC Name |
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide |
| Synonym |
Copanlisib |
| Solubility |
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 µL 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 µL 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. 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. |
| Appearance |
Faint Pink-Purple Powder |
Glauer J, Pletz N, Schön M, et al. A novel selective small-molecule PI3K inhibitor is effective against human multiple myeloma in vitro and in vivo. Blood Cancer J. 2013 Sep 6;3:e141. PMID: 24013662.
Cheng H, Merika E, Syrigos KN, et al. Novel agents for the treatment of pancreatic adenocarcinoma. Highlights from the “2011 ASCO Annual Meeting”. Chicago, IL, USA; June 3-7, 2011. JOP. 2011 Jul 8;12(4):334-8. PMID: 21737890.
