Filgotinib (GLPG0634)
中文名称：菲戈替尼
Filgotinib (GLPG0634)是一个选择性JAK1抑制剂，其对JAK1, JAK2, JAK3,和TYK2的IC50分别为10 nM, 28 nM, 810 nM,和116 nM。Phase 2。
Filgotinib (GLPG0634) Chemical Structure
CAS: 1206161-97-8
产品质控
批次：
纯度：
99.76%
99.76
Filgotinib (GLPG0634)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human CD34+ cells | Function assay | 45 mins | Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis | 24417533 | |
| NK92 | Function assay | Inhibition of JAK1/JAK3 in IL2-induced human NK92 cells assessed as pSTAT5, =0.148μM. | 25369270 | ||
| THP1 | Function assay | Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6, =0.154μM. | 25369270 | ||
| U2OS | Function assay | Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1, =0.436μM. | 25369270 | ||
| HeLa | Function assay | Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter, =1.045μM. | 25369270 | ||
| THP1 | Function assay | Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1, =3.364μM. | 25369270 | ||
| TF1 | Function assay | Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5, =3.524μM. | 25369270 | ||
| BaF3 | Function assay | Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation, =4.546μM. | 25369270 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Filgotinib (GLPG0634)是一个选择性JAK1抑制剂，其对JAK1, JAK2, JAK3,和TYK2的IC50分别为10 nM, 28 nM, 810 nM,和116 nM。Phase 2。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在细胞系中，GLPG0634抑制IL-2和IL-4诱导的JAK1/JAK3/γc信号和IFN-αB2诱导的JAK1/TYK2 II型受体信号，IC50值范围为150 到760 nM。GLPG0634对JAK/STAT信号中JAK1激酶比对JAK2激酶在细胞水平上显示出更高的选择性。此外，GLPG0634也会抑制Th1，Th2，和Th17细胞的分化。[1] | |||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-STAT3 / STAT3 |
|
28191885 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 口服给药后，大鼠体内的绝对生物利用度适中(45%)，而小鼠体内很高(∼100%)。在大鼠和小鼠CIA模型中，Filgotinib (30 mg/kg 每天 (大鼠)；50 mg/kg一天两次 (小鼠))剂量依赖性减少炎症，软骨，和骨退化现象。[1] Filgotinib (GLPG0634)在DSS处理的小鼠体内研究表明，JAK1的抑制在临床前小鼠模型中足以实现强的疗效，在发炎的结肠中与STAT3磷酸化的抑制相关。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 大鼠 CIA 模型和小鼠 CIA 模型 |
| Dosages | 30 mg/kg 每天 (大鼠)；50 mg/kg 每天两次 (小鼠) | |
| Administration | p.o. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06222034 | Recruiting | Juvenile Idiopathic Arthritis |
Galapagos NV |
April 2024 | Phase 1 |
| NCT06043739 | Completed | Bioavailability |
Galapagos NV |
September 22 2023 | Phase 1 |
| NCT05697159 | Recruiting | Rheumatoid Arthritis|Sickness Behavior|Inflammatory Disease|Autoimmune|Pain Chronic |
NHS Greater Glasgow and Clyde|Galapagos NV |
August 22 2023 | -- |
| NCT05653791 | Active not recruiting | Ulcerative Colitis |
Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Galapagos NV |
October 1 2022 | -- |
| NCT03417778 | Completed | Rheumatoid Arthritis |
Gilead Sciences|Galapagos NV |
April 3 2018 | Phase 1 |
化学信息&溶解度
| 分子量 | 425.50 | 分子式 | C21H23N5O3S |
| CAS号 | 1206161-97-8 | SDF | Download Filgotinib (GLPG0634) SDF |
| Smiles | C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 21 mg/mL ( (49.35 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
Could you recommemd a vehicle for oral gavage for S7605?
回答：
It can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension for oral gavage.
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