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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-TAK-279
TAK-279

Chemical Structure : TAK-279

CAS No.: 2272904-53-5

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TAK-279 (Zasocitinib, TAK279, NDI-034858)

货号: PC-20516Not For Human Use, Lab Use Only.

NDI-034858 (Zasocitinib, TAK-279) is a potent, selective and allosteric TYK2 inhibitor, targets TYK2 JH2 domain with binding KD of 3.8 pM.

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2 mg ￥1880 In stock
5 mg ￥3280 In stock
10 mg ￥5280 In stock
25 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAK-279 (Zasocitinib, NDI-034858) is a potent, selective and allosteric TYK2 inhibitor, targets TYK2 JH2 domain with binding KD of 3.8 pM.
TAK-279 exhibites hignly potent cellular pSTAT4 IL12 PBMC IC50 of 6.7 nM.
TAK-279 displays functional selectivity over JAK1, JAK2, and JAK3.
TAK-279 inhibits IFNα-stimulated phosphorylation of STAT3 in CD3-positive T-cells as well as IFNα-stimulated CXCL10 production in whole blood with IC50s of 1.7 and 22 nM, respectively.
TAK-279 inhibits IL23-stimulated phosphorylation of STAT3 in human CD161 + CD3 + TH17 cells with an IC50 of 3.7 nM.
TAK-279 inhibits IFNα-stimulated CXCL10 production  in mouse and rat whole blood with IC50 of 347 and 91 nM, respectively.
TAK-279 also inhibits IL12-IL18-stimulated induction of IFNγ in whole blood with IC50 of 48 nM.
TAK-279 (30 mg/kg) demonstrated dose-dependent suppression of IL12/IL18-induced IFNγ production in rat in vivo PD model.

物理化学性质&存储条件

分子量 460.50
分子式 C23H24N8O3
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

N-((1R,2R)-2-methoxycyclobutyl)-7-(methylamino)-5-((2-oxo-2H-[1,2'-bipyridin]-3-yl)amino)pyrazolo[1,5-a]pyrimidine-3-carboxamide

参考文献

1. Patent WO2019023468 A1. Pyrazolopyrimidines as TYK2 inhibitors and their preparation.
2. Leit S, et al. J Med Chem. 2023 Jul 10. doi: 10.1021/acs.jmedchem.3c00600.

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