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Copanlisib dihydrochloride

(Synonyms: BAY 80-6946 dihydrochloride)
36 Cited Publications
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Based on 36 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

  • Purity: 99.55%
  • CAS No.: 1402152-13-9
  • Formula: C23H30Cl2N8O4
  • Molecular Weight:553.44
  • Storage:

    4°C, sealed storage, away from moisture

    * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

  • Copanlisib dihydrochloride Chemical Structure
    Copanlisib dihydrochloride Chemical Structure
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
  • Experimental Validation Results for Copanlisib dihydrochloride
CAS No.: 1402152-13-9
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Apoptosis AnalysisRT-PCRCell Imaging/StainingWBCell Proliferation/Viability AssayIn Vivo Efficacy Study
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  • Copanlisib dihydrochloride Chemical Structure
    Copanlisib dihydrochloride Chemical Structure
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    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]

    Customer Validation
     Apoptotic WCM3409 PDTOs were quantified in the presence of α-PD-1 after Copanlisib (Copanlisib dihydrochloride; EC10 0.005 μM-EC25 0.021 μM; 3-day pretreatment followed by 1-day co-culture). The addition of Copanlisib increased killing levels in the presence of α-PD-1 and α-PD-1 plus α-TIM3 (5 μg/ml) for WCM3409.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2025 Oct 6. [Abstract]

    Customer Validation
     Representative western blot analysis of selected PI3K downstream target proteins in HN30R8 and HN31P10 cisplatin-resistant HNSCC cells after Copanlisib (Copanlisib dihydrochloride; 5-1000 nM; 6 h), with β-actin as a loading control. Acute exposure to Copanlisib did not significantly inhibit AKT phosphorylation but reduced the phosphorylation of p70 S6, 4E-BP1 and S6.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]

    Customer Validation
     Western blot analysis of Akt, p-Akt (Ser473), p-Akt (Thr308), and cleaved caspase 3/8 expression after 6 h of treatment with copanlisib (2 nM, pan-PI3K inhibitor) and GEM treatment.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]

    Customer Validation
     Colony formation by cells overexpressing cFAM124A after 6 h of treatment with different inhibitors and GEM treatment in 6-well dishes (800 cells/well) for 2 weeks. Each inhibitor, Copanlisib (2 nM, pan-PI3K inhibitor) or K-80003 (5 nM, tRXRα-dependent Akt activation inhibitor).

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]

    Customer Validation
     Subcutaneous xenograft model of mice in the different groups treated with GEM (40 mg/kg i.p. 2×/week for 4 weeks), Copanlisib (1 mg/kg, iv. 2×/week for 4 weeks), or K-80003 (20 mg/ kg i.p. 2×/week for 4 weeks) at 2 weeks after subcutaneous injection of 5 × 106 cells overexpressing cFAM124A and control cells.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Front Oncol. 2022 Sep 8:12:944537. [Abstract]

    Customer Validation
     MTT results and combination index (CI) plots evaluated Huh7 lenvatinib-resistant (Huh7 LR) cell viability after Copanlisib (Copanlisib dihydrochloride; 12.5-25 nM; 96 h) alone or in combination with lenvatinib. Copanlisib significantly enhanced the inhibitory effect of lenvatinib on Huh7 LR cell proliferation.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Front Oncol. 2022 Sep 8:12:944537. [Abstract]

    Customer Validation
     Micrographs showed the morphology of Huh7 lenvatinib-resistant (Huh7 LR) cells after Copanlisib (Copanlisib dihydrochloride; 3 μM; 72 h) alone or in combination with lenvatinib. Copanlisib enhanced the pro-apoptotic effect of lenvatinib in Huh7 LR cells.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Front Oncol. 2022 Sep 8:12:944537. [Abstract]

    Customer Validation
     Flow cytometry plots showed apoptosis in Huh7 LR cells after copanlisib (Copanlisib dihydrochloride; 3 μM; 72 h) alone or in combination with lenvatinib. Copanlisib significantly enhanced the pro-apoptotic effect of lenvatinib.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]

    Customer Validation
     Induction of apoptosis after 96-hour exposure to DMSO, Entospletinib (ENTO, 2 μM), Ibrutinib (IBRU, 0.1 μM), Copanlisib (COPA, 0.25 μM), or Pictilisib (PICTI, 0.5 μM) shown as percentage of annexin V/PI-positive cells plus or minus SEM from at least 3 biological replicates.

  • 1/16

    Copanlisib dihydrochloride purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]

    Customer Validation
     HRK, BCL-xL, BFL-1, or BIM transcript abundance after 24-hour exposure to DMSO, Entospletinib (2 μM), Ibrutinib (0.1 μM), Copanlisib (0.25 μM), or Pictilisib (0.5 μM) was determined with RT-qPCR relative to PPIA.

  • Copanlisib dihydrochloride