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

Copanlisib  (Synonyms: BAY 80-6946)

Cat. No.: HY-15346 Purity: 99.50%
COA Handling Instructions

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.

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

Copanlisib Chemical Structure

Copanlisib Chemical Structure

CAS No. : 1032568-63-0

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Copanlisib:

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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].

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

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].

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.
Clinical Trial
Molecular Weight

480.52

Appearance

Solid

Formula

C23H28N8O4
CAS No.
SMILES

O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 20 mg/mL (41.62 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1M HCl

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.50%

COA (245 KB) RP-HPLC (173 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • 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.

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Keywords:

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

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