计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
JAK3-IN-1
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC 50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC 50 of 896 nM) and JAK2 (IC 50 of 1050 nM)
In Vitro
JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. .\nJAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC 50 = 13 nM), TTK protein kinase (TTK, IC 50 = 49 nM), BLK proto-oncogene (BLK, IC 50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC 50 = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC 50 s against EGFRWT and TYK2 (IC 50 s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC 50 s for BTK or ITK (IC 50 s = 794 and 1070 nM respectively). JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC 50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: BMDMs cells Concentration: 0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM Incubation Time: 3 hours Result: Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.
In Vivo
JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T 1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%.\nAfter oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:JAK3 4.8 nM (IC 50 ) JAK1 896 nM (IC 50 ) JAK2 1050 nM (IC 50 ) TTK 49 nM (IC 50 ) BTK 794 nM (IC 50 ) ITK 1070 nM (IC 50 )
规格
规格或纯度
Moligand™,10mM in DMSO
英文名称
JAK3-IN-1
生化机理
JAK3-IN-1 是一种强效、选择性和口服活性 JAK3 抑制剂，其 IC 50 为 4.8 nM。与 JAK1（IC 50 为 896 nM）和 JAK2（IC 50 为 1050 nM）相比，JAK3-IN-1 对 JAK3 的选择性高出 180 多倍。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NCC4=CC(=CC=C4)NC(=O)C=C)Cl)OC
PubChem CID
分子量
508.02
技术文档
高级数据
关联靶点（人）
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(1 活性数据)
JAK3
Tclin
酪氨酸蛋白激酶JAK3(Tyrosine-protein kinase JAK3)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）