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CAS: 202475-60-3
分子式: C16H15N3O3
分子量: 297.31
中文名称: 
4-(4'-羟基苯基)氨基-6,7-二甲氧基喹唑啉
英文名称: 
janex-1
whi-p131
whi-p 131
用途: JANEX-1 是一种有效的特异性 JAK3 抑制剂,Ki 为 2.3 μM,IC50 为 78 μM,JANEX-1 不抑制 JAK1 和 JAK2。
推荐供应商
货号品牌产品名称规格包装、参考价格
W793882MACKLIN4-(4\'-羟基苯基)氨基-6, 7-二甲氧基喹唑啉10mM in DMSO648元/1ml;   咨询
储存:-20°C
W860951MACKLIN4-(4\'-羟基苯基)氨基-6,7-二甲氧基喹唑啉>98%198元/10mg;   405元/50mg;   761元/250mg;   2273元/1g;   咨询
储存:-20℃
状态:浅黄色固体
折射率:light yellow solid
1563401J&KJANEX-198%, 一种有效的特异性 JAK3 抑制剂902元/5MG;   1608元/10MG;   咨询

基本信息

分子式C16H15N3O3
分子量297.31
存储条件Freezer -20℃

产品描述

JANEX-1是JAK3小分子抑制剂,选择性抑制JAK3,IC50为78 μM。它不影响JAK1或JAK2,及其他蛋白酪氨酸激酶的活性(IC50 ≥ 350 µM)。

靶点(IC50 & Targe)

JAK3,Ki:2.3μM

体外研究

JANEX-1 inhibits JAK3 but not JAK1 or JAK2. The ZAP/SYK family tyrosine kinase SYK, TEC family tyrosine kinase Bruton’s tyrosine kinase (BTK), SRC family tyrosine kinase LYN, and receptor family tyrosine kinase insulin receptor kinase (IRK) are not inhibited by JANEX-1[1]. JANEX-1 suppresses IL-1β and IFN-γ-induced phosphorylation of STAT-1, STAT-3, and STAT-5 proteins. JANEX-1 has a potent inhibitory effect on cytokine-induced β-cell damage[2].

体内研究

JANEX-1 is very well tolerated by mice and monkeys and effective plasma concentrations of JANEX-1 could be achieved at nontoxic dose levels. JANEX-1 suppresses the mitogen and antigen responses of T-cells and attenuates the severity of T-cell-dependent graft-versus-host disease in a bone marrow transplantation model[1].

动物实验

Animal Models: Female NOD mice

Formulation: DMSO in PBS

Dosages: 20, 50 and 100 mg/kg/day

Administration: IP

(Only for Reference)

参考文献

[1] Cetkovic-Cvrlje M, et al. Clin Immunol. 2003, 106(3):213-25.

[2] Lv N, et al. Exp Cell Res. 2009, 315(12):2064-71.

安全信息

图形或危害标志
危险说明H302
H410
防范说明P264
P270
P273
P301+P312
P330
P391
P501
UN号码3077
危险分类9
包装等级III
420101Sigma-AldrichJAK3 Inhibitor I-CAS 202475-60-3-CalbiochemThe JAK3 Inhibitor I, also referenced under CAS 202475-60-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation appli2741.8元/5 MG;   咨询

产品说明

一般描述

A cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3; IC50 = 78 µM). Has no effect on JAK1, JAK2, or Zap/Syk or Src tyrosine kinases. Acts as a potent inhibitor of glioblastoma cell adhesion and migration. Also reported to block thrombin-induced platelet aggregation.
A cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3) (IC50 = 78 µM). Has no effect on either JAK1, JAK2, Zap/Syk or Src kinases. Blocks thrombin-induced platelet aggregation.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
Janus family kinase 3
Target IC50: 78 µM against Janus family kinase 3
Product competes with ATP.
Reversible: yes

警告

Toxicity: Standard Handling (A)

其他说明

Tibbles, H.E., et al. 2001. J. Biol. Chem.276, 17815.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res.5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin. Cancer Res. 4, 2463.

法律信息

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

基本信息

经验(实验)分子式C16H15N3O3
分子量297.31

产品性质

质量水平100
测定≥97% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white to off-white
溶解性DMSO: 50 mg/mL
运输ambient
储存温度−20℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 1
闪点(F)Not applicable
闪点(C)Not applicable
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