2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：1402152-13-9 Product 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. EINECS: Molecular Formula：C23H30Cl2N8O4 Molecular Weight：553.44
Target:
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.
Kinase Assay
Cell Assay
Animal Administration
References
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
