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    Copanlisib (BAY80-6946; Aliqopa)
    Copanlisib  (BAY80-6946; Aliqopa)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0136
    CAS #: 1032568-63-0 Purity ≥98%

    Description: Copanlisib (formerly BAY 80-6946; brand name: Aliqopa) is a potent, ATP-competitive and pan-class I PI3K (phosphoinositide 3-kinase) inhibitor with potential anticancer activity. It has IC50s of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ, respectively. As of September 2017, Copanlisib was approved by FDA for the treatment of adult patients experiencing relapsed follicular lymphoma who have received at least two prior systemic therapies. BAY 80-6946 showed high anti-proliferative activity with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines. BAY 80-6946 is generally well tolerated through the maximum tolerated dose (MTD) of 0.8 mg/kg. pharmacokinetics (PK) results support dosing weekly. Grade 2 or 3 hyperglycemia in the first 24 hrs after receiving a MTD dose. Pharmacokinetics, clinical SD as well as FDG-PET data are consistent with effective exposure and PI3K pathway inhibition. 

    References: Mol Cancer Ther. 2013 Nov;12(11):2319-30; Breast Cancer Res Treat. 2015 Jan;149(2):373-83.

    Related CAS: 1402152-13-9 (HCl); 1402152-46-8 (HCl hydrate)  

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    Molecular Weight (MW)

    480.52

    Formula

    C23H28N8O4

    CAS No.

    1032568-63-0 (free base); 

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: <1 mg/mL

    Water:<1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    10% Trifluoroacetic acid water solution: 1mg/mL 

    Other info

    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.

    Synonyms

    Aliqopa; BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; 


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    In Vitro

    In vitro: In both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells.

    Kinase Assay: The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of 33P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp® plates coated with 2 µg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 µL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl2, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 µL of a 40-µM ATP solution containing 20 µCi/mL [33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 µL of a 25-mM EDTA solution. The plates are washed and Ultima Gold™ scintillation cocktail (25 µL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter. 

    Cell Assay: Cell proliferation over a 72-hour period is determined using the CellTiter-Glo® luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37ºC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37ºC. Luminescence values are determined with a Wallac 1420 Victor2™ 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo® solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.

    In Vivo

    In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition.

    Animal model

    Rats bearing KPL4 or HCT116 xenografts 

    Formulation & Dosage

    Formulated in PEG400/acidified water (0.1 N HCl, pH 3.5; 20/80, v/v) or 5% mannitol; 6 mg/kg; i.v. 

    References

    Mol Cancer Ther. 2013 Nov;12(11):2319-30; Breast Cancer Res Treat. 2015 Jan;149(2):373-83.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    BAY 80-6946 (Copanlisib)

    Activity of BAY 80-6946 in xenograft models using an every second day (Q2D) schedule. Mol Cancer Ther. 2013, 12(11), 2319-2330.

    BAY 80-6946 (Copanlisib)

    Activity of BAY 80-6946 in xenograft models using a twice a day (BID) once-weekly schedule.

    BAY 80-6946 (Copanlisib)

    Antiproliferative IC50 values of BAY 80-6946 in cancer cell lines from various indications with gene mutation status


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