- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
Filgotinib (GLPG0634)
中文名稱：菲戈替尼
Filgotinib (GLPG0634)是一個(gè)選擇性JAK1抑制劑，其對(duì)JAK1, JAK2, JAK3,和TYK2的IC50分別為10 nM, 28 nM, 810 nM,和116 nM。Phase 2。
Filgotinib (GLPG0634) Chemical Structure
CAS: 1206161-97-8
產(chǎn)品質(zhì)控
批次：
純度：
99.76%
99.76
Filgotinib (GLPG0634)相關(guān)產(chǎn)品
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Filgotinib (GLPG0634)是一個(gè)選擇性JAK1抑制劑，其對(duì)JAK1, JAK2, JAK3,和TYK2的IC50分別為10 nM, 28 nM, 810 nM,和116 nM。Phase 2。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在細(xì)胞系中，GLPG0634抑制IL-2和IL-4誘導(dǎo)的JAK1/JAK3/γc信號(hào)和IFN-αB2誘導(dǎo)的JAK1/TYK2 II型受體信號(hào)，IC50值范圍為150 到760 nM。GLPG0634對(duì)JAK/STAT信號(hào)中JAK1激酶比對(duì)JAK2激酶在細(xì)胞水平上顯示出更高的選擇性。此外，GLPG0634也會(huì)抑制Th1，Th2，和Th17細(xì)胞的分化。[1] | |||
|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | p-STAT3 / STAT3 |
|
28191885 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 口服給藥后，大鼠體內(nèi)的絕對(duì)生物利用度適中(45%)，而小鼠體內(nèi)很高(～100%)。在大鼠和小鼠CIA模型中，F(xiàn)ilgotinib (30 mg/kg 每天 (大鼠)；50 mg/kg一天兩次 (小鼠))劑量依賴性減少炎癥，軟骨，和骨退化現(xiàn)象。[1] Filgotinib (GLPG0634)在DSS處理的小鼠體內(nèi)研究表明，JAK1的抑制在臨床前小鼠模型中足以實(shí)現(xiàn)強(qiáng)的療效，在發(fā)炎的結(jié)腸中與STAT3磷酸化的抑制相關(guān)。[2] | |
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 大鼠 CIA 模型和小鼠 CIA 模型 |
| Dosages | 30 mg/kg 每天 (大鼠)；50 mg/kg 每天兩次 (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 |
|
化學(xué)信息&溶解度
| 分子量 | 425.50 | 分子式 | C21H23N5O3S |
| CAS號(hào) | 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 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 21 mg/mL ( (49.35 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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* 必填項(xiàng)
常見問題及建議解決方法
問題 1:
Could you recommend a vehicle for oral gavage for it?
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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