1. GPCR/G Protein PI3K/Akt/mTOR
  2. Adenosine Receptor PI3K
  3. CGS 15943

CGS 15943 

Cat. No.: HY-100678 Purity: 99.96%
COA Handling Instructions

CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

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

CGS 15943 Chemical Structure

CGS 15943 Chemical Structure

CAS No. : 104615-18-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 157 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 157 In-stock
Solid
1 mg USD 50 In-stock
5 mg   Get quote  
10 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. [1][2].

IC50 & Target

p110γ

1.1 μM (IC50)

p110δ

8.47 μM (IC50)

adenosine A1 receptor

3.5 nM (Ki)

adenosine A2A receptor

4.2 nM (Ki)

adenosine A2B receptor

16 nM (Ki)

adenosine A3 receptor

50 nM (Ki)

In Vitro

CGS 15943 inhibits the kinase activity of the class IB PI3K isoform p110γ with an IC50 of 1.1 μM and shows slight inhibition on p110δ with an IC50 of 8.47 μM[3].
CGS 15943 (0-20 μM; 72 hours) inhibits growth of HLF and SK-Hep-1 cells, as well as HepG2 and PLC-PRF-5 cells[3].
CGS 15943 (0-20 μM; 24 hours) reduces the phosphorylation of Akt at its residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells[3].

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

Cell Viability Assay[3]

Cell Line: HLF, SK-Hep-1, HepG2 and PLC-PRF-5 cells
Concentration: 0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 24 hours
Result: Inhibited growth of four distinct HCC cell lines.

Western Blot Analysis[3]

Cell Line: HLF and Sk-Hep-1 cells
Concentration: 0 μM; 1 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 24 hours
Result: Inhibited the PI3K/Akt pathway in HLF and Sk-Hep-1 cells
Molecular Weight

285.69

Appearance

Solid

Formula

C13H8ClN5O

CAS No.
SMILES

NC1=NC2=C(C=C(Cl)C=C2)C3=NC(C4=CC=CO4)=NN13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.22 mg/mL (42.77 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5003 mL 17.5015 mL 35.0030 mL
5 mM 0.7001 mL 3.5003 mL 7.0006 mL
10 mM 0.3500 mL 1.7501 mL 3.5003 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.22 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.22 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.22 mg/mL (4.27 mM); Clear solution

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

Purity: 99.96%

References
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CGS 15943 Related Classifications

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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This equation is commonly abbreviated as: C1V1 = C2V2

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Product Name:
CGS 15943
Cat. No.:
HY-100678
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