2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. Copanlisib dihydrochloride

Copanlisib dihydrochloride  (Synonyms: BAY 80-6946 dihydrochloride)

Cat. No.: HY-15346A Purity: 99.55%
COA
SDS
Handling Instructions Technical Support

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.

CAS No. : 1402152-13-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of Copanlisib dihydrochloride:

Copanlisib dihydrochloride Related Antibodies

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Copanlisib dihydrochloride

Apoptosis Analysis
RT-PCR
WB
Cell Proliferation/Viability Assay
In Vivo Efficacy Study

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

    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.

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

    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).

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

    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.

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

    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.

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

    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.

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    IC50 & Target[1]

    PI3Kα

    0.5 nM (IC50)

    PI3Kδ

    0.7 nM (IC50)

    PI3Kβ

    3.7 nM (IC50)

    PI3Kγ

    6.4 nM (IC50)

    mTOP

    45 nM (IC50)

    In Vitro

    Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab[1].
    Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells[1].
    Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Copanlisib dihydrochloride Related Antibodies

    Apoptosis Analysis[1]

    Cell Line: BT20 breast cancer cells
    Concentration: 20 nM and 62 nM, 200 nM
    Incubation Time: 24 hours
    Result: Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC50 of 340 nM.

    Western Blot Analysis[1]

    Cell Line: ELT3 cells
    Concentration: 0.5 nM, 5 nM, 50 nM, 500 nM
    Incubation Time: 2 hours
    Result: Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.
    In Vivo

    Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic nude rats injected with KPL4 tumor cells[1]
    Dosage: 0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg
    Administration: Intravenous injection; every second day, every third day; for 60 days
    Result: On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.
    Molecular Weight

    553.44

    Formula

    C23H30Cl2N8O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (90.34 mM; Need ultrasonic)

    DMSO : 5 mg/mL (9.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8069 mL 9.0344 mL 18.0688 mL
    5 mM 0.3614 mL 1.8069 mL 3.6138 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (180.69 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.55%

    SDS (419 KB)

    COA (247 KB) HNMR (196 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.8069 mL 9.0344 mL 18.0688 mL 45.1720 mL
    5 mM 0.3614 mL 1.8069 mL 3.6138 mL 9.0344 mL
    H2O 10 mM 0.1807 mL 0.9034 mL 1.8069 mL 4.5172 mL
    15 mM 0.1205 mL 0.6023 mL 1.2046 mL 3.0115 mL
    20 mM 0.0903 mL 0.4517 mL 0.9034 mL 2.2586 mL
    25 mM 0.0723 mL 0.3614 mL 0.7228 mL 1.8069 mL
    30 mM 0.0602 mL 0.3011 mL 0.6023 mL 1.5057 mL
    40 mM 0.0452 mL 0.2259 mL 0.4517 mL 1.1293 mL
    50 mM 0.0361 mL 0.1807 mL 0.3614 mL 0.9034 mL
    60 mM 0.0301 mL 0.1506 mL 0.3011 mL 0.7529 mL
    80 mM 0.0226 mL 0.1129 mL 0.2259 mL 0.5647 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Copanlisib dihydrochloride Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Copanlisib1402152-13-9BAY 80-6946PI3KApoptosisPhosphoinositide 3-kinaseAKTphosphorylationantitumorintravenousadministrationsub-nanomolarantiproliferativeInhibitorinhibitorinhibit

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