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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Delgocitinib
Delgocitinib

Chemical Structure : Delgocitinib

CAS No.: 1263774-59-9

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Delgocitinib (JTE052;JTE-052;LEO 124249;LEO124249)

货号: PC-60508Not For Human Use, Lab Use Only.

Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively.
Delgocitinib (JTE-052, LEO 124249) does not inhibit a broad panel of kinases with exception of ROCK-II (IC50=140 nM).
Delgocitinib (JTE-052, LEO 124249) inhibits cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage CSF, and IFN-α in vitro.
Delgocitinib (JTE-052, LEO 124249) potently suppresses the IL-2-induced IFN-γ production in mice (ED50=1.1 mg/kg), suppresses inflammatory responses in collagen-induced arthritis model.
 

物理化学性质&存储条件

分子量 310.361
分子式 C16H18N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)- 1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile

参考文献

1. Tanimoto A, et al. Inflamm Res. 2015 Jan;64(1):41-51.

2. Amano W, et al. J Allergy Clin Immunol. 2015 Sep;136(3):667-677.e7.

3. Tanimoto A, et al. BMC Musculoskelet Disord. 2015 Nov 6;16:339.

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