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Submit ReviewAS 2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor (IC50 = 21 nM). Displays 30-fold selectivity for IRAK4 over IRAK1. Inhibits LPS-induced TNF-α and IL-6 production in PBMCs in vitro. Renoprotective and anti-inflammatory in a rodent model of chronic kidney disease.
AS 2444697 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 432.86 |
公式 | C19H20N6O4.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1287665-60-4 |
PubChem ID | 118719434 |
InChI Key | FGNHLIIFEDYNFZ-UHFFFAOYSA-N |
Smiles | O=C(N)C2=NN(C=C2NC(C3=COC(C4=CC=NC(C)=C4)=N3)=O)C1CCOCC1.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 8.66 | 20 温和加热 |
以下数据基于产品分子量 432.86。 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 |
---|---|---|---|
0.2 mM | 11.55 mL | 57.76 mL | 115.51 mL |
1 mM | 2.31 mL | 11.55 mL | 23.1 mL |
2 mM | 1.16 mL | 5.78 mL | 11.55 mL |
10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
参考文献是支持产品生物活性的出版物。
Chaudhary (2015) Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders. J.Med.Chem. 58 96 PMID: 25479567
Kondo et al (2014) Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch.Pharmacol. 387 909 PMID: 25052043
Schmaderer and Heemann (2014) Blocking innate immunity to slow the progression of chronic kidney disease. Naunyn Schmiedebergs Arch.Pharmacol. 387 905 PMID: 25107563
If you know of a relevant reference for AS 2444697, please let us know.
关键词: AS 2444697, AS 2444697 supplier, AS2444697, potent, selective, interleukin-1, receptor-associated, kinase, 4, IRAK4, inhibitors, inhibits, anti-inflammatory, renoprotective, Cytokines, IRAK, 5430, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AS 2444697 的部分引用包括:
Zhang et al (2018) Tumor-Stroma IL1β-IRAK4 Feedforward Circuitry Drives Tumor Fibrosis, Chemoresistance, and Poor Prognosis in Pancreatic Cancer. Cancer Res 78 1700 PMID: 29363544
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