CGS 15943

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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