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

Copanlisib  (Synonyms: BAY 80-6946)

製品番号: HY-15346 純度: 99.35%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 1032568-63-0

容量 価格（税別） 在庫状況 数量
5 mg $60 在庫あり
10 mg $90 在庫あり
25 mg $168 在庫あり
50 mg $270 在庫あり
100 mg $450 在庫あり
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500 mg   お問い合わせ  

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カスタマーレビュー

Based on 34 publication(s) in Google Scholar

Other Forms of Copanlisib:

Copanlisib 関連抗体

Top Publications Citing Use of Products

顧客検証

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

    Copanlisib 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 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 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 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 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.

    PI3K アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Copanlisib (BAY 80-6946) 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 has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib 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)

    mTOR

    45 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.12 μM
    Compound: Copanlisib
    Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 32069401]
    HCT-116 IC50
    0.13 μM
    Compound: Copanlisib
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    		[PMID: 36586298]
    HT-29 IC50
    0.93 μM
    Compound: Copanlisib
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    		[PMID: 36586298]
    HT-29 IC50
    0.95 μM
    Compound: Copanlisib
    Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 32069401]
    HUVEC IC50
    34.75 μM
    Compound: Copanlisib
    Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    		[PMID: 36586298]
    HUVEC IC50
    35.42 μM
    Compound: Copanlisib
    Cytotoxicity against HUVEC assessed as reduction in cell viability
    Cytotoxicity against HUVEC assessed as reduction in cell viability
    		[PMID: 32069401]
    LoVo IC50
    0.053 μM
    Compound: Copanlisib
    Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 32069401]
    LoVo IC50
    0.06 μM
    Compound: Copanlisib
    Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method
    		[PMID: 36586298]
    MCF7 IC50
    0.01 μM
    Compound: Copanlisib
    Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 32069401]
    体外実験

    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) 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 関連抗体

    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.
    体内実験

    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.
    臨床実験
    分子量

    480.52

    分子式

    C23H28N8O4
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    1 M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)

    DMSO : 5 mg/mL (10.41 mM; ultrasonic and adjust pH to 5 with HCl; 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 2.0811 mL 10.4054 mL 20.8108 mL
    5 mM 0.4162 mL 2.0811 mL 4.1622 mL
    10 mM 0.2081 mL 1.0405 mL 2.0811 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    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:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (10.41 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

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    (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
    純度とドキュメンテーション

    純度: 99.35%

    COA (245 KB) HNMR (192 KB) RP-HPLC (257 KB) MS (68 KB) Elemental Analysis Report (103 KB)

    取扱説明書 (2659 KB)
    参考文献

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / 1 M HCl 1 mM 2.0811 mL 10.4054 mL 20.8108 mL 52.0270 mL
    5 mM 0.4162 mL 2.0811 mL 4.1622 mL 10.4054 mL
    10 mM 0.2081 mL 1.0405 mL 2.0811 mL 5.2027 mL
    1 M HCl 15 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4685 mL
    20 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
    25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0811 mL
    30 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    40 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3007 mL
    50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
    60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
    100 mM 0.0208 mL 0.1041 mL 0.2081 mL 0.5203 mL
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    Copanlisib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      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:

    Copanlisib1032568-63-0BAY 80-6946PI3KApoptosisPhosphoinositide 3-kinaseAKTphosphorylationantitumorintravenousadministrationsub-nanomolarantiproliferativeInhibitorinhibitorinhibit

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    製品名:
    Copanlisib
    製品番号:
    HY-15346
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