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Copanlisib dihydrochloride

Catalog No. T14998   CAS 1402152-13-9
Synonyms: BAY 80-6946 dihydrochloride

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ). Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Copanlisib dihydrochloride Chemical Structure
Copanlisib dihydrochloride, CAS 1402152-13-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 72.00
25 mg In stock $ 128.00
50 mg In stock $ 222.00
100 mg In stock $ 372.00
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Purity: 99.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ). Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
Targets&IC50 mTOR:45 nM, PI3Kγ:6.4 nM, PI3Kα:0.5 nM, PI3Kβ:3.7 nM, PI3Kδ:0.7 nM
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. [1] 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. [2]
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. [1]
Synonyms BAY 80-6946 dihydrochloride
Molecular Weight 553.44
Formula C23H30Cl2N8O4
CAS No. 1402152-13-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

H2O: 20 mg/mL, Sonication is recommended.

TargetMolReferences and Literature

1. Liu N, et al. Mol Cancer Ther. 2013, 12(11), 2319-2330. 2. Elster N, et al. Breast Cancer Res Treat. 2015, 149(2), 373-383.

TargetMolCitations

1. Xiong W, Jia L, Cai Y, et al.Evaluation of the anti-inflammatory effects of PI3Kδ/γ inhibitors for treating acute lung injury.Immunobiology.2023: 152753.

Related compound libraries

This product is contained In the following compound libraries:
FDA-Approved Kinase Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library HIF-1 Signaling Pathway Compound Library Drug-induced Liver Injury (DILI) Compound Library

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Keywords

Copanlisib dihydrochloride 1402152-13-9 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR Inhibitor antiproliferative inhibit intravenous BAY 80-6946 sub-nanomolar Copanlisib BAY 80-6946 dihydrochloride BAY 80-6946 Dihydrochloride phosphorylation Copanlisib Dihydrochloride Phosphoinositide 3-kinase AKT antitumor administration inhibitor

 

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