Home Cart Sign in  
Chemical Structure| 1032568-63-0 Chemical Structure| 1032568-63-0
Chemical Structure| 1032568-63-0

Copanlisib

CAS No.: 1032568-63-0

Copanlisib is a potent and highly selective reversiblePI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.

Synonyms: BAY 80-6946

4.5 *For Research Use Only !

Cat. No.: A199526 Purity: 98%

Change View

Size Price

US Stock

Global Stock

In Stock
2mg łÇÿ¶ÊÊ Inquiry Inquiry
5mg łËÿ¶ÊÊ Inquiry Inquiry
10mg ł§ÿ¶ÊÊ Inquiry Inquiry
25mg łÿď¶ÊÊ Inquiry Inquiry
50mg łóͶÊÊ Inquiry Inquiry
100mg łÇÍ˶ÊÊ Inquiry Inquiry
250mg łËËó¶ÊÊ Inquiry Inquiry
1g łòËÿ¶ÊÊ Inquiry Inquiry

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 2mg

    łÇÿ¶ÊÊ

  • 5mg

    łËÿ¶ÊÊ

  • 10mg

    ł§ÿ¶ÊÊ

  • 25mg

    łÿď¶ÊÊ

  • 50mg

    łóͶÊÊ

  • 100mg

    łÇÍ˶ÊÊ

  • 250mg

    łËËó¶ÊÊ

  • 1g

    łòËÿ¶ÊÊ

In Stock

- +

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support Online Technical Q&A
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.

Purchased from AmBeed:

Alternative Products

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 Vitro:

Cell Line
Concentration Treated Time Description Reference
Human kidney cells (HK2) 100 nM 16 hours Copanlisib reduced aberrant actin polymerization in OCRL-deficient HK2 cells, rescuing the actin-endosomal overlap. PMC7550850
MINO cells 0.05 µM 72 hours To evaluate the antiproliferative effect of ASN007 in combination with Copanlisib, results showed that the combination significantly enhanced antitumor activity PMC8324497
AC1 cells 100 nM 24 hours To evaluate the effect of Copanlisib on cell proliferation and apoptosis, results showed that Copanlisib had no significant effect on the proliferation and survival of AC1 cells. PMC10192075
SC1 cells 100 nM 24 hours To evaluate the effect of Copanlisib on cell proliferation and apoptosis, results showed that Copanlisib had no significant effect on the proliferation and survival of SC1 cells. PMC10192075
Calu3 cells 10 nM 3 days To evaluate the effect of Copanlisib on phospho-AKT levels in Calu3 cells, results showed that Copanlisib significantly reduced phospho-AKT levels. PMC8743034
Sw1573 cells 10 nM 3 days To evaluate the effect of Copanlisib on phospho-AKT levels in Sw1573 cells, results showed that Copanlisib significantly reduced phospho-AKT levels. PMC8743034
A549 cells 10 nM Copanlisib synergistically inhibited the downstream Bcl-2 with siPGRN PMC9485207
H520 cells 10 nM Copanlisib reversed the upregulation of p-Akt and Bcl-2 by PGRN protein PMC9485207
DLD1 100 nM 24 hours To evaluate the apoptosis-inducing effect of Copanlisib on DLD1 cells, the results showed that Copanlisib significantly increased the apoptotic rate. PMC7606528
ATL cell lines 1 µM 2 hours and 4 hours To evaluate the effect of Copanlisib on ATL cell lines, results showed that Copanlisib reduced the expression of p-AKT and p-4EBP1. PMC9006306
ATL43T b(-) cell line 125 nM 72 hours To evaluate the effect of Copanlisib in combination with I-BET762 on the ATL43T b(-) cell line, results showed that the combination significantly reduced cell viability. PMC9006306

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice MINO xenograft model Intraperitoneal injection 400 μmol/kg Single dose To evaluate the in vivo antitumor effect of ASN007 in combination with Copanlisib, results showed that the combination significantly delayed tumor growth PMC8324497
Mice PTEN/p53-deficient prostate cancer model Intravenous injection 14 mg/kg 2 days on, 5 days off, continued To evaluate the inhibitory effect of Copanlisib alone or in combination with ADT on tumor growth, results showed that Copanlisib alone or in combination with ADT significantly inhibited tumor growth and increased the activation and phagocytic activity of tumor-associated macrophages. PMC10192075
Mice PTEN/p53-deficient prostate cancer model Intravenous injection 1 mg kg−1 Once daily for 7 days To evaluate the tumor growth control effect of Copanlisib monotherapy, results showed a 37.5% overall response rate. PMC10841690
Nude mice Calu3 xenograft model Intraperitoneal injection 25 mg/kg Administered every two days for 7 days To evaluate the effect of Copanlisib alone or in combination with EPZ6438 on tumor growth in Calu3 xenograft model, results showed that combination therapy significantly inhibited tumor growth. PMC8743034
Nu/Nu mice HCT116 xenograft model Intraperitoneal injection 14 mg/kg Every other day for 28 days To evaluate the antitumor effect of Copanlisib in the HCT116 xenograft model, the results showed that Copanlisib significantly inhibited tumor growth. PMC7606528
NSG mice ATL43T b(-) xenograft model Intraperitoneal injection 40 mg/kg Once daily for 7 days To evaluate the effect of Copanlisib in combination with I-BET762 on the ATL43T b(-) xenograft model, results showed that the combination significantly inhibited tumor growth and prolonged the survival of mice. PMC9006306

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

 

Historical Records

Categories