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Merck
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主要文件

420097

Sigma-Aldrich

Janus蛋白酪氨酸激酶(JAK)抑制剂I

InSolution, ≥98%

别名:

InSolution JAK抑制剂I, 2-（1，1-二甲基乙基）-9-氟-3，6-二氢-7H-苯并[h]-咪唑[4，5-f]异喹啉-7-酮，P6，吡啶酮6，DBI，JAK1抑制剂I，JAK2抑制剂I，JAK3抑制剂X

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About This Item

经验公式（希尔记法）:
C18H16FN3O
CAS号:
457081-03-7
分子量:
309.34
MDL编号:
MFCD17019334
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

liquid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

运输

wet ice

储存温度

2-8°C

SMILES字符串

Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1

InChI

1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)

InChI key

VNDWQCSOSCCWIP-UHFFFAOYSA-N

一般描述

Janus蛋白酪氨酸激酶（JAKs）的有效抑制剂。显示对JAK1（对于鼠JAK1，IC50=15 nM）、JAK2（IC50=1 nM）、JAK3（Ki=5 nM）和Tyk2（IC50=1 nM）的有效抑制活性。它仅在高得多的浓度下抑制其他激酶。还抑制CTLL细胞的IL-2和IL-4依赖性增殖，并阻断STAT5的磷酸化。

生化/生理作用

5 nM，针对JAK3
主要靶标
鼠JAK1
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：分别针对鼠JAK1和JAK2的15 nM，1 nM；针对Tyk2为1 nM

包装

用惰性气体包装

警告

毒性：刺激性（B）

外形

10 mM（500 µg/162 µl）JAK抑制剂I（目录号420099）的DMSO溶液。

重悬

初次使用后，等分并冷藏（4°C）。

其他说明

Thompson, J.E., et al. 2002.Bioorg.Med. Chem. Lett.12, 1219.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

10 - Combustible liquids

WGK

WGK 2

闪点(°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

闪点(°C)

87 °C - closed cup - (Dimethylsulfoxide)

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