Binding Mode
ChemicalBook > CAS DataBase List > BAY 80-6946 (Copanlisib)

BAY 80-6946 (Copanlisib)

Binding Mode
Product Name
BAY 80-6946 (Copanlisib)
CAS No.
1032568-63-0
Chemical Name
BAY 80-6946 (Copanlisib)
Synonyms
Copanlisib;BAY80-6946;CS-2321;Aliqopa);Copanlisib base;Copanlisib free base;Copanlisib(BAY80-6946);BAY 80-6946 (BAY80-6946;BAY 80-6946 (Copanlisib);BAY 80-6946 (Copanlisib) USP/EP/BP
CBNumber
CB52616024
Molecular Formula
C23H28N8O4
Formula Weight
480.52
MOL File
1032568-63-0.mol
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BAY 80-6946 (Copanlisib) Property

Density 
1.51
storage temp. 
Store at -20°C
solubility 
insoluble in DMSO; insoluble in H2O; insoluble in EtOH
form 
solid
pka
8.42±0.20(Predicted)
color 
Off-white to light brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
20354
Product name
Copanlisib
Purity
≥98%
Packaging
5mg
Price
$61
Updated
2024/03/01
Cayman Chemical
Product number
20354
Product name
Copanlisib
Purity
≥98%
Packaging
1mg
Price
$72
Updated
2023/06/20
Cayman Chemical
Product number
20354
Product name
Copanlisib
Purity
≥98%
Packaging
10mg
Price
$91
Updated
2024/03/01
TRC
Product number
B119060
Product name
BAY80-6946
Packaging
10mg
Price
$395
Updated
2021/12/16
Biosynth Carbosynth
Product number
BC164810
Product name
Copanlisib
Packaging
25mg
Price
$450
Updated
2021/12/16
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BAY 80-6946 (Copanlisib) Chemical Properties,Usage,Production

Binding Mode

As shown in the co-crystal structure of copanlisib bound to PI3Kγ, the inhibitor binds with only one critical hydrogen bond to the amide NH of Val882 in the adenine pocket, employing the imidazoline N1 nitrogen (Figs. 1 and 2). In addition, the C5 aminopyrimidine group fills the affinity pocket, forming hydrogen bonds with two carboxylic residues of Asp836 and Asp841 through the amino group. Finally, the solvent exposed morpholine lies over Trp812, presumably providing additional attractive molecular contacts.

Uses

BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models.

Definition

ChEBI: Copanlisib is an imidazoquinazoline that is 2,3-dihydroimidazo[1,2-c]quinazoline substituted by (2-aminopyrimidine-5-carbonyl)amino, methoxy, and 3-(morpholin-4-yl)propoxy groups at positions 5, 7 and 8, respectively. It is a intravenous pan-class I PI3K inhibitor used for the treatment of relapsed follicular lymphoma in patients who have received at least 2 prior systemic therapies. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of morpholines, an aromatic ether, a diether, a tertiary amino compound, a secondary carboxamide, a pyrimidinecarboxamide, an aminopyrimidine and an imidazoquinazoline.

brand name

Aliqopa

General Description

Class: lipid kinase; Treatment: FL (IV infusion); Other name: BAY 80-6946; Elimination half-life = 52 h (IV); Protein binding = 84.2%

Pharmacokinetics

Copanlisib has poor oral bioavailability due to low permeability and poor solubility, and therefore, it is not suitable for an oral medication. Consequently, it was developed as an IV drug. IV infusion of copanlisib resulted in rapid distribution throughout the body and a prolonged elimination half-life (52 h).

target

pan-PI3K

Metabolism

Copanlisib was the predominant component in human plasma, accounting for 84% of total radioactivity AUC, and the morpholinone metabolite 6 was the only circulating metabolite (about 5%).

BAY 80-6946 (Copanlisib) Preparation Products And Raw materials

Raw materials

Preparation Products

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BAY 80-6946 (Copanlisib) Suppliers

MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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United States
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Cckinase, Inc.
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BOC Sciences
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Aladdin Scientific
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TargetMol Chemicals Inc.
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United States Biological
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View Lastest Price from BAY 80-6946 (Copanlisib) manufacturers

Career Henan Chemical Co
Product
BAY 80-6946 (Copanlisib) 1032568-63-0
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

1032568-63-0, BAY 80-6946 (Copanlisib)Related Search:


  • BAY 80-6946 (Copanlisib)
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  • BAY 80-6946; BAY80-6946; BAY-80-6946; BAY806946; BAY-806946; BAY 806946; COPANLISIB FREE BASE
  • Copanlisib free base
  • BAY 80-6946 (Copanlisib) USP/EP/BP
  • Aliqopa)
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  • 1032568-63-0
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  • Inhibitors
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