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Copanlisib (dihydrochloride)

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

Product Specifications

CAS Number

[1402152-13-9]

Product Name Alternative

BAY 80-6946 (dihydrochloride)

UNSPSC

12352005

Hazard Statement

H360, H372

Target

Apoptosis; PI3K

Type

Reference compound

Related Pathways

Apoptosis; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/copanlisib-dihydrochloride.html

Purity

99.55

Solubility

DMSO : 5 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25.[H]Cl.[H]Cl

Molecular Formula

C23H30Cl2N8O4

Molecular Weight

553.44

Precautions

H360, H372

References & Citations

[1]Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12 (11) :2319-30.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ

Citation 01

BioRxiv. 2025 Jan 16:2025.01.10.632413.|Br J Cancer. 2025 Oct 6.|Front Oncol. 2022 Sep 8:12:944537.|Bioorg Chem. 2025 Apr 5:160:108424.|Blood Adv. 2022 Apr 12;6 (7) :2346-2360.|Blood. 2019 Jan 3;133 (1) :70-80.|Br J Cancer. 2025 Oct 6.|Breast Cancer Res Treat. 2020 Jan;179 (2) :337-347.|Cancer Discov. 2025 Jan 13;15 (1) :202-226.|Cancer Lett. 2022 Jan 1:524:151-160.|Carbohydr Polym. 2024 Feb 15:326:121637.|Cell Biosci. 2020 Feb 12;10:16.|Cell Biosci. 2022 Aug 2;12 (1) :122.|Cell Biosci. 2022 Dec 30;12 (1) :210.|Front Immunol. 2021 Oct 15;12:699478.|Front Oncol. 2021 Jul 13:11:704042.|Genes Dis. 2021 Jul 1;9 (6) :1650-1661.|J Clin Invest. 2021 Dec 15;131 (24) :e140436.|J Immunother Cancer. 2022 Mar;10 (3) :e003402.|J Oncol. 2022 Apr 29;2022:1515416.|Mol Cancer Ther. 2025 Jul 10.|Mol Cancer. 2023 Mar 30;22 (1) :64.|Mol Cancer. 2024 Sep 30;23 (1) :215.|Mol Carcinog. 2024 Apr 17|Mol Syst Biol. 2024 Jan;20 (1) :28-55.|Nat Cancer. 2024 Aug;5 (8) :1250-1266.|RSC Adv. 2019 Feb 21;9 (11) :6409-6418.|Sci Rep. 2025 Aug 10;15 (1) :29265.|Science. 2017 Dec 1;358 (6367) :eaan4368.|Signal Transduct Target Ther. 2025 Oct 31;10 (1) :356.|Theranostics. 2020 Jan 1;10 (4) :1531-1543.|Université de Lausanne. 2024 Feb 7.

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