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

Chemical Structure : Lepzacitinib

CAS No.: 2321488-47-3

Lepzacitinib (ATI-1777, ATI 1777)

货号: PC-21734Not For Human Use, Lab Use Only.

Lepzacitinib (ATI-1777) is a potent, selective and ATP-competitive JAK1/3 inhibitor with IC50 of 1.5/3.6/7.1/19.0 nM for JAK1/JAK2/JAK3/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

Lepzacitinib (ATI-1777) is a potent, selective and ATP-competitive JAK1/3 inhibitor with IC50 of 1.5/3.6/7.1/19.0 nM for JAK1/JAK2/JAK3/TYK2, respectively.
ATI-1777 displays 32 to 833 fold selectivity for Jak1/3 over a panel of 214 human protein kinases.
ATI-1777 demonstrates inhibition of STAT phosphorylation in isolated PBMCs with IC50 of 19 nM, 5-fold selectivity over Jak1/2 and approximately 42- to 47-fold selectivity over Jak2.
ATI-1777 application inhibits IL-15–induced CCL8 expression in pig skin by 83%, selectively inhibits Jak1/3 with limited systemic exposure and without any adverse effects.

物理化学性质&存储条件

分子量 355.40
分子式 C18H21N5O3
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

ethyl (R)-4-((1-(2-cyanoacetyl)piperidin-3-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxylate

参考文献

1. Changelian P, et al. JID Innov. 2023 Nov 28;4(2):100251.

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