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Chemical Structure| 1032568-63-0 Chemical Structure| 1032568-63-0

Structure of Copanlisib
CAS No.: 1032568-63-0

Chemical Structure| 1032568-63-0

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Copanlisib is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.

Synonyms: BAY 80-6946

4.5 *For Research Use Only !

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Product Citations

Product Citations

Verena Haage ; John F. Tuddenham ; Natacha Comandante-Lou ; Alex Bautista ; Anna Monzel ; Rebecca Chiu , et al.

Abstract: While efforts to identify microglial subtypes have recently accelerated, the relation of transcriptomically defined states to function has been largely limited to in silico annotations. Here, we characterize a set of pharmacological compounds that have been proposed to polarize human microglia towards two distinct states – one enriched for AD and MS genes and another characterized by increased expression of antigen presentation genes. Using different model systems including HMC3 cells, iPSC-derived microglia and cerebral organoids, we characterize the effect of these compounds in mimicking human microglial subtypes in vitro. We show that the Topoisomerase I inhibitor Camptothecin induces a CD74high/MHChigh microglial subtype which is specialized in amyloid beta phagocytosis. Camptothecin suppressed amyloid toxicity and restored microglia back to their homeostatic state in a zebrafish amyloid model. Our work provides avenues to recapitulate human microglial subtypes in vitro, enabling functional characterization and providing a foundation for modulating human microglia in vivo.

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Product Details of Copanlisib

CAS No. :1032568-63-0
Formula : C23H28N8O4
M.W : 480.52
SMILES Code : O=C(C1=CN=C(N)N=C1)NC2=NC3=C(C=CC(OCCCN4CCOCC4)=C3OC)C5=NCCN25
Synonyms :
BAY 80-6946
MDL No. :MFCD18633201
InChI Key :MWYDSXOGIBMAET-UHFFFAOYSA-N
Pubchem ID :135565596

Safety of Copanlisib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Copanlisib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:6.4 nM

  • p110β

    PI3Kβ, IC50:3.7 nM

  • p110α

    PI3Kα, IC50:0.5 nM

  • p110δ

    PI3Kδ, IC50:0.7 nM

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Balb/C mice Intravenous 5.0 mg/kg Single dose Pharmacokinetic study, Enasidenib used as internal standard for quantification of copanlisib in mice plasma ADMET DMPK. 2020 Mar 4;8(1):113-121

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04433182 Diffuse Large B-cell Lymphoma PHASE2 TERMINATED 2024-12-19 Ospedale Monsignor Raffaele Di... More >>miccoli - Ematologia, Barletta, Barletta-Andria-Trani, Italy|Centro Riferimento Oncologico - S.O.C. Oncologia Medica A, Aviano, Pordenone, Italy|Ematologia, Candiolo Cancer Institute. FPO-IRCCS, Candiolo, Torino, 10060, Italy|AOU Ospedali Riuniti - Clinica di Ematologia, Ancona, Italy|ASST Spedali Civili - Ematologia, Brescia, Italy|Arnas Nuovo Ospedale Garibaldi Nesima - U.O.C. Ematologia, Catania, Italy|A.O. S. Croce e Carle - S.C. di Ematologia e Trapianto di Midollo Osseo, Cuneo, Italy|Ospedale Vito Fazzi - Ematologia, Lecce, Italy|Azienda Ospedali Riuniti Papardo-Piemonte - S.C. Ematologia, Messina, Italy|I.R.C.C.S. Istituto Oncologico Veneto - Oncologia 1, Padova, Italy|AOU Policlinico Giaccone - Ematologia, Palermo, Italy|IRCCS Policlinico S. Matteo di Pavia - Divisione di Ematologia, Pavia, Italy|Ospedale Guglielmo da Saliceto - U.O.Ematologia, Piacenza, Italy|Azienda Ospedaliera Sant'Andrea - Ematologia, Roma, Italy|Policlinico Umberto I - Università "La Sapienza" Istituto Ematologia -Dipartimento di Medicina Traslazionale e di Precisione, Roma, Italy|Azienda Ospedaliera S. Maria di Terni - S.C. Oncoematologia, Terni, Italy|Azienda Ospedaliero Universitaria Città della Salute e della Scienza - S.C.Ematologia, Torino, Italy|Ospedale Ca' Foncello - S.C di Ematologia, Treviso, Italy Less <<
NCT04803123 Leukemia, Acute Lymphocytic EARLY_PHASE1 TERMINATED 2023-04-26 Duke Cancer Center, Durham, No... More >>rth Carolina, 27710, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.41mL

2.08mL

1.04mL

20.81mL

4.16mL

2.08mL

References

 

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