JAK-IN-1|1334673-53-8|-陌孚医药/Medlife

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JAK-IN-1

目录号: PL03728 纯度: ≥99%

CAS No. :1334673-53-8

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中文名称	JAK-IN-1
中文别名	n-[(1r)-1-[(3-氰基-1-氮杂啶)羰基]-2,2-二甲基丙基]-2-环丙基-5H-吡咯并[2,3-b]吡嗪-7-羧酰胺
英文名称	JAK-IN-1
英文别名	5H-pyrrolo[2,3-b]pyrazine-7-carboxamide, n-[(1r)-1-[(3-cyano-1-azetidinyl)carbonyl]-2,2-dimethylpropyl]-2-cyclopropyl-;JAK-IN-1;BDBM50426601;5H-Pyrrolo[2,3-b]pyrazine-7-carboxaMide,N-[(1R)-1- [(3-cyano-1-azetidinyl)carbonyl]-2,2-diMethylpropyl]-2-cyclopropyl-
Cas No.	1334673-53-8
分子式	C₂₀H₂₄N₆O₂
分子量	380.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	JAK-IN-1是 JAK1/2/3 抑制剂， IC₅₀ 分别为0.26，0.8 和3.2 nM。JAK-IN-1对JAK3的选择性比JAK1高。
生物活性	JAK-IN-1 is a JAK1/2/3 inhibitor with IC 50 s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
性状	Solid
IC50 & Target[1][2]	IC50: 0.26 nM (JAK1), 0.8 nM (JAK2), 3.2 nM (JAK3)
体外研究(In Vitro)	JAK-IN-1 inhibits the proliferation of human CD4 and CD8 T cells in a dose-dependent manner upon stimulation by anti-CD3/anti-CD28 antibody-coated beads partially mimicking the activation signals brought to a Tcell by an antigen-presenting cell. JAK-IN-1 is active in both mechanistic and functional cell-based assays using T-cells, one of the major cell types in which JAK3 is potentially relevant. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	JAK-IN-1 is JAK3 selective in vivo, as judged by higher potency inhibiting JAK1/JAK3- vs JAK2- or JAK1/JAK2/TYK2-driven signaling in whole blood assays. JAK-IN-1 potently inhibits IL-2 stimulated plasma concentrations of JAK-IN-1 for each dose. JAK-IN-1 prevents IL-2-driven STAT5 phosphorylation in a dose- and concentration-dependent manner, with approximately 50% inhibition observed at the 10 mg/kg dose (plasma concentration ～480 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Soth M, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem. 2013 Jan 10;56(1):345-56.

溶解度数据	In Vitro: DMSO : 66.67 mg/mL (175.24 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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