Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewCGS 15943
说明： Potent adenosine receptor antagonist
化学名： 9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
纯度： ≥99% (HPLC)
生物活性 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.
技术数据 for CGS 15943
| 分子量 | 285.69 |
| 公式 | C13H8ClN5O |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CGS 15943
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 1.43 | 5 |
制备储备液 for CGS 15943
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
产品说明书 for CGS 15943
参考文献 for CGS 15943
参考文献是支持产品生物活性的出版物。
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.
按产品操作查看相关产品
关键词: CGS 15943, CGS 15943 supplier, Potent, adenosines, receptor, antagonists, Non-Selective, Receptors, CGS15943, Non-selective, Adenosine, PI, 3-Kinase, 1699, Tocris Bioscience
7 篇 CGS 15943 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CGS 15943 的部分引用包括：
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
Ilie et al (2012) Adenosine release during seizures attenuates GABAA receptor-mediated depolarization. J Neurosci 32 5321 PMID: 22496577
Sivaramakrishnan et al (2012) Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes. J Cell Sci 125 4567 PMID: 22767503
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
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
Diógenes et al (2014) Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase. Cereb Cortex 24 67 PMID: 22997174
您是否知道使用了 Tocris CGS 15943 的优秀论文？ 请告知我们.
CGS 15943 的评论
平均评分: 5 (Based on 1 Review.)
Have you used CGS 15943?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Filter by:
In vivo and in vitro use of CGS 15943.
By
Ariel Vitenzon on 01/05/2018
分析类型： In Vivo
种属： Mouse
细胞系/组织： 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.