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| | Copanlisib Basic information |
| Product Name: | Copanlisib | | Synonyms: | Copanlisib HCl;copanlisib hydrochloride;Copanlisib HCI;2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide;Copanlisib.2HCl;COPANLISIB HCL; COPANLISIB DIHYDROCHLORIDE; BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; COPANLISIB; TRADE NAME ALIQOPA.;trade name Aliqopa.;BAY 80-6946 dihydrochloride | | CAS: | 1402152-13-9 | | MF: | C23H29ClN8O4 | | MW: | 516.99 | | EINECS: | | | Product Categories: | | | Mol File: | 1402152-13-9.mol |  |
| | Copanlisib Chemical Properties |
| solubility | DMSO:1.0(Max Conc. mg/mL);2.08(Max Conc. mM)
Water:0.67(Max Conc. mg/mL);1.39(Max Conc. mM) | | form | Solid | | color | Off-white to light yellow |
| | Copanlisib Usage And Synthesis |
| Uses | 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]. | | Definition | ChEBI: Copanlisib dihydrochloride is the dihydrochloride salt of copanlisib. It has a role as an antineoplastic agent, an apoptosis inducer and an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It contains a copanlisib. | | 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.
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| | IC 50 | PI3Kα: 0.5 nM (IC50); PI3Kδ: 0.7 nM (IC50); PI3Kβ: 3.7 nM (IC50); PI3Kγ: 6.4 nM (IC50); mTOP: 45 nM (IC50) | | References | [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. DOI:10.1158/1535-7163.MCT-12-0993-T |
| | Copanlisib Preparation Products And Raw materials |
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