Cat. No.: HY-100678

CGS 15943

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

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Pureté: 99.55%
CAS No.: 104615-18-1
Formule: C₁₃H₈ClN₅O
Masse moléculaire:285.69

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CGS 15943 Chemical Structure

CAS No.: 104615-18-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1][2]

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)

Voir tous les produits spécifiques à Isoform Adenosine Receptor :

Voir tous les produits spécifiques à Isoform PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1.2 μM Compound: 1a	Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor	[PMID: 9667972]
CHO	IC₅₀	406 nM Compound: CGS-15943	Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor Inhibition of cAMP accumulation in CHO cells expressing human adenosine A3 receptor	[PMID: 11123985]

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].

MedChemExpress (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

Chemical Information

CAS No. 104615-18-1
Appearance Solid
Masse moléculaire 285.69
Formule C₁₃H₈ClN₅O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 12.22 mg/mL (42.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

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

This protocol yields a suspended solution of 1.22 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a suspended solution of 1.22 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 1.22 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.2 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Gao Y, et al. CGS 15943, an adenosine A2 receptor antagonist, reduces cerebral ischemic injury in the Mongolian gerbil. Life Sci. 1994;55(3):PL61-5. [Content Brief]

[2]. Klotz KN, et al. Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91. [Content Brief]

[3]. Edling CE, et al. Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol Ther. 2014 May;15(5):524-32. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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 mM	3.5003 mL	17.5015 mL	35.0030 mL	87.5074 mL
	5 mM	0.7001 mL	3.5003 mL	7.0006 mL	17.5015 mL
	10 mM	0.3500 mL	1.7501 mL	3.5003 mL	8.7507 mL
	15 mM	0.2334 mL	1.1668 mL	2.3335 mL	5.8338 mL
	20 mM	0.1750 mL	0.8751 mL	1.7501 mL	4.3754 mL
	25 mM	0.1400 mL	0.7001 mL	1.4001 mL	3.5003 mL
	30 mM	0.1167 mL	0.5834 mL	1.1668 mL	2.9169 mL
	40 mM	0.0875 mL	0.4375 mL	0.8751 mL	2.1877 mL

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CGS 15943

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Voir tous les produits spécifiques à Isoform Adenosine Receptor

Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CGS 15943 Related Classifications

HY-100678 Related Classifications