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Copanlisib dihydrochloride (BAY 80-6946)

  Cat. No.:  DC28978   Featured
Chemical Structure
1402152-13-9
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More than 5000 active chemicals with high quality for research!
Field of application
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1402152-13-9
Chemical Name: 5-Pyrimidinecarboxamide, 2-amino-N-(2,3-dihydro-7-methoxy-8-(3-(4-morpholinyl)propoxy)imidazo(1,2-C)quinazolin-5-yl)-, hydrochloride (1:2)
Synonyms: Copanlisib HCl; Copanlisib dihydrochloride; BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; Copanlisib; trade name Aliqopa.
SMILES: O=C(NC1N2C(=NCC2)C2C(=C(C(=CC=2)OCCCN2CCOCC2)OC)N=1)C1C=NC(N)=NC=1.[H]Cl.[H]Cl
Formula: C23H30Cl2N8O4
M.Wt: 553.44
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Liu N, et al. 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.
Description: Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity[1].
In Vivo: Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model[1]. Animal Model: Athymic nude rats injected with KPL4 tumor cells[1] Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg Administration: Intravenous injection; every second day, every third day; for 60 days Result: On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.
In Vitro: Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1]. Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells[1]. Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[1]. Apoptosis Analysis[1] Cell Line: BT20 breast cancer cells Concentration: 20 nM and 62 nM, 200 nM Incubation Time: 24 hours Result: Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC50 of 340 nM. Western Blot Analysis[1] Cell Line: ELT3 cells Concentration: 0.5 nM, 5 nM, 50 nM, 500 nM Incubation Time: 2 hours Result: Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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