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> Copanlisib [1032568-63-0]

Copanlisib [1032568-63-0]

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Référence HY-15346-5mg

Conditionnement : 5mg

Marque : MedChemExpress

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Description

Copanlisib (BAY 80-6946) 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 has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity[1].

IC50 & Target[1]

PI3Kα

0.5 nM (IC50)

PI3Kδ

0.7 nM (IC50)

PI3Kβ

3.7 nM (IC50)

PI3Kγ

6.4 nM (IC50)

mTOR

45 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.12 μM
Compound: Copanlisib
Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 32069401]
HCT-116 IC50
0.13 μM
Compound: Copanlisib
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
[PMID: 36586298]
HT-29 IC50
0.93 μM
Compound: Copanlisib
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
[PMID: 36586298]
HT-29 IC50
0.95 μM
Compound: Copanlisib
Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 32069401]
HUVEC IC50
34.75 μM
Compound: Copanlisib
Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
[PMID: 36586298]
HUVEC IC50
35.42 μM
Compound: Copanlisib
Cytotoxicity against HUVEC assessed as reduction in cell viability
Cytotoxicity against HUVEC assessed as reduction in cell viability
[PMID: 32069401]
LoVo IC50
0.053 μM
Compound: Copanlisib
Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 32069401]
LoVo IC50
0.06 μM
Compound: Copanlisib
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
[PMID: 36586298]
MCF7 IC50
0.01 μM
Compound: Copanlisib
Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 32069401]
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) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Copanlisib Related Antibodies

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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Essai clinique
Masse moléculaire

480.52

Formule

C23H28N8O4
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

1 M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)

DMSO : 5 mg/mL (10.41 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0811 mL 10.4054 mL 20.8108 mL
5 mM 0.4162 mL 2.0811 mL 4.1622 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (10.41 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
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