CGS 15943

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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)
Citations (7)
Reviews (1)

Biological Activity for CGS 15943

CGS 15943 is a potent adenosine receptor antagonist (Ki values are 3.5, 4.2, 16 and 51 nM for human A1, A2A, A2B 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
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 Data for CGS 15943

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 mL 70.01 mL 140.01 mL
0.5 mM 7 mL 35 mL 70.01 mL
2.5 mM 1.4 mL 7 mL 14 mL

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Product Datasheets for CGS 15943

Certificate of Analysis / Product Datasheet
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References for CGS 15943

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

Ghai et al (1987) Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 242 784 PMID: 3656113

Klotz (2000) Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 362 382 PMID: 11111832

Williams et al (1987) Biochemical characterization of the triazoloquinazoline CGS 15943, a novel, non-xanthine adenosine antagonist. J.Pharmacol.Exp.Ther. 241 415 PMID: 2883298

Wesseler et al (2022) Phenotypic discovery of triazolo[1,5-c]quinazolines as a first-in-class bone morphogenetic protein amplifier chemotype. J.Med.Chem. 65 15263 PMID: 36346705

Shropshire et al (2022) Association of adenosine signaling gene signature with estrogen receptor-positive breast and prostate cancer bone metastasis. Front.Med. (Lausanne) 9 965429 PMID: 36186774

Edling et al (2014) Caffeine and the analog CGS 15943 inhibit cancer cell growth by targeting the phosphoinositide 3-kinase/Akt pathway. Cancer Biol.Ther. 15 524 PMID: 24521981

If you know of a relevant reference for CGS 15943, please let us know.

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Keywords: CGS 15943, CGS 15943 supplier, Potent, adenosines, receptor, antagonists, Non-Selective, Receptors, CGS15943, Non-selective, Adenosine, PI, 3-Kinase, 1699, Tocris Bioscience

7 Citations for CGS 15943

Citations are publications that use Tocris products. Selected citations for CGS 15943 include:

Peng et al (2016) Purinergic and store-operated Ca(2+) signaling mechanisms in mesenchymal stem cells and their roles in ATP-induced stimulation of cell migration. Stem Cells 34 2102 PMID: 27038239

Avanzato et al (2016) Activation of P2X7 and P2Y11 purinergic receptors inhibits migration and normalizes tumor-derived endothelial cells via cAMP signaling Scientific Reports 6 32602 PMID: 27586846

Wakisaka et al (2017) An Adenosine Receptor for Olfaction in Fish. Curr Biol 27 1437 PMID: 28502661

Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448

Do you know of a great paper that uses CGS 15943 from Tocris? Please let us know.

Reviews for CGS 15943

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In vivo and in vitro use of CGS 15943.
By Ariel Vitenzon on 01/05/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: systemic

This compound was used both in vivo and in vitro. For in vivo experiments we injected the compound systemically into transgenic mice and evaluated the effect of the drug on motor behavior. In vitro we used the drug on slices to evaluate the effect on the physiology of cells.

Drug was dissolved using saline + 0.3% tween 80. (Vortexed for 1 minute and sonicated for 5 min) X3 times.