CGS 15943

Name: CGS 15943
Brand: Tocris Bioscience
SKU: 1699
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1699

(1)

Citations (61)

COA / SDS

Potent adenosine receptor antagonist

Key Product Details

Description:	Potent adenosine receptor antagonist
Chemical Name:	9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
Purity:	≥99% (HPLC)
Molecular Weight:	285.69

View Full Technical Details for CGS 15943

Technical Data
Citations / Reviews (1)

Biological Activity for CGS 15943

CGS 15943 is a potent adenosine receptor antagonist (K_i values are 3.5, 4.2, 16 and 51 nM for human A₁, A_2A, A_2B and A₃ receptors respectively). Inhibits the catalytic subunit of the class IB PI3K isoform p110γ (IC₅₀ = 1.1 μM). Blocks HCC and HDAC cell proliferation in vitro via inhibition of the PI3K/Akt pathway; reduces proliferation of ER⁺ breast cancer cells. Also acts as a BMP-4 mimetic to stimulate osteogenic differentiation. Orally active in vivo.

Technical Data for CGS 15943

M. Wt	285.69
Formula	C₁₃H₈ClN₅O
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	104615-18-1
PubChem ID	122070
InChi Key	JLPYLHLUHJOPNL-UHFFFAOYSA-N
Smiles	NC1=NC2=CC=C(Cl)C=C2C2=NC(=NN12)C1=CC=CO1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CGS 15943

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	1.43	5

Preparing Stock Solutions for CGS 15943

The following data is based on the product molecular weight 285.69.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.05 mM	70.01 mL	350.03 mL	700.06 mL
0.25 mM	14.00 mL	70.01 mL	140.01 mL
0.5 mM	7.00 mL	35.00 mL	70.01 mL
2.5 mM	1.40 mL	7.00 mL	14.00 mL

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References for CGS 15943

References are publications that support the biological activity of the product.

Edling Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol.Ther. 2014 PMID: 24521981
Shropshire Association of adenosine signaling gene signature with estrogen receptor-positive breast and prostate cancer bone metastasis. Front.Med. (Lausanne) 2022 PMID: 36186774
Wesseler Phenotypic discovery of triazolo[1,5-c]quinazolines as a first-in-class bone morphogenetic protein amplifier chemotype. J.Med.Chem. 2022 PMID: 36346705
Williams Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 1987 PMID: 2883298
Klotz Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 2000 PMID: 11111832
Ghai Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 1987 PMID: 3656113