Filgotinib (GLPG0634)

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

Filgotinib (GLPG0634)化学構造

CAS No. 1206161-97-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 44800 国内在庫なし(納期7~10日)
JPY 21400 国内在庫あり
JPY 44600 国内在庫なし(納期7~10日)
JPY 144200 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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Filgotinib (GLPG0634)関連製品

シグナル伝達経路

JAK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
Targets
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
10 nM 28 nM 116 nM 810 nM
In Vitro
In vitro In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells. [1]
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-STAT3 / STAT3 28191885
In Vivo
In Vivo Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. [1] Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon. [2]
動物実験 動物モデル Rat CIA model and mouse CIA model
投与量 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
投与経路 p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

化学情報

分子量 425.50 化学式

C21H23N5O3S

CAS No. 1206161-97-8 SDF Download Filgotinib (GLPG0634) SDFをダウンロードする
Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5
保管

In vitro
Batch:

DMSO : 21 mg/mL ( (49.35 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問(FAQ)

質問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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