IRAK4-IN-7
产品说明书
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同义名 : | CA-4948;IRAK4-IN-2 |
| CAS号 : | 1801343-74-7 | |
| 货号 : | A345196 | |
| 分子式 : | C21H19N7O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 417.421 | |
| MDL号 : | MFCD31619276 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(28.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Interleukin-1 Receptor Associated Kinase-4 (IRAK-4) is a serine/threonine protein kinase belonging to tyrosine like kinase (TLK) family. It is one of the important signalling components downstream of IL-1/Toll family of receptors (IL-1R, IL-18R, IL-33R, Toll-like receptors) and plays a critical role in initiating innate immune response against foreign pathogens. Involved in Toll-like receptor (TLR) and IL-1R signaling pathways, IRAK-4 is rapidly recruited by MYD88 to the receptor-signaling complex upon TLR activation to form the Myddosome together with IRAK2.CA-4948, previously termed AU-4948, is a selective and potent IRAK4 inhibitor. According to data obtained from enzymatic assays, the inhibitory IC50 value of CA-4948 against human IRAK4 kinase is 37 nM. Moreover, CA-4948 showed high selectivity towards IRAK4 with kinase selectivity S35 score of 0.0343 at 1 μM. In vitro, CA-4948 inhibited ABC DLBCL OCI-LY10, SUDHL-2 and U2932 cells’ viability with IC50 values of 3.58 μM, 7.86 μM and 10.42 μM, respectively. The treatment time was 72 h, and cell viability was determined by a CellTiter-Glo method. In western blot analysis of a DLBCL cell line during a 20 min TLR-agonist stimulation, CA-4948 suppressed the phosphorylation level of IKK-β, NF-kB p65, and JNK at the concentration of 10 μM[1]. In ABC DLBCL OCI-LY3 xenograft model, CA-4948 administrated orally at the doses of 50 mg/kg or 150 mg/kg daily for more than 15 days resulted in tumor growth inhibition of 53% and 49%, respectively[1]. | ||
| 作用机制 | CA-4948 is a potent and selective IRAK4 kinase inhibitor. According to docking mode study, CA-4948 anticipated to bind in ATP binding pocket close to gate-keeper Tyr262 residue in human IRAK4[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
11.98mL 2.40mL 1.20mL |
23.96mL 4.79mL 2.40mL |
| 参考文献 |
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