Filgotinib (GLPG0634)

Catalog No.S7605

For research use only.

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) Chemical Structure

CAS No. 1206161-97-8

Selleck's Filgotinib (GLPG0634) has been cited by 35 publications

Purity & Quality Control

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Biological Activity

Description 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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells NYnQPJE6TnWwY4Tpc44h[XO|YYm= Mom2OFUhdWmwcx?= NXfwNIFLUW6qaXLpeIlwdiCxZjDKRWszKGixbX;kbY1meiCrbjDoeY1idiCFREO0L{Bk\WyuczDzdIls\WRiaX70c{BpfW2jbjD3bI9t\SCkbH;v[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWStOUBxcG:|cHjvdplt[XSrb36gdJJmcW6ldXLheIVlKG[xcjC0OUBucW6|IH\vcIxwf2WmIHL5JGVRVyCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KE[DQ2OgZY5idHm|aYO= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{WzN{c,OjR2MUe1N|M9N2F-
NK92 M1;YdWZ2dmO2aX;uJIF{e2G7 NIjIUJFKdmirYnn0bY9vKG:oIFrBT|EwUkGNMzDpckBKVDJvaX7keYNm\CCqdX3hckBPUzl{IHPlcIx{KGG|c3Xzd4VlKGG|IIDTWGFVPSxiPUCuNVQ5|ryPLh?= NUPj[mdJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlkzPzBpPkK1N|Y6OjdyPD;hQi=>
THP1 MVXGeY5kfGmxbjDhd5NigQ>? M{Wx[GlvcGmkaYTpc44hd2ZiSlHLNU9LSUt|IHnuJGlNPC2rbnT1Z4VlKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNicGPURXQ3NCB;MD6xOVTPxE1w M3\K[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{[5NlcxLz5{NUO2PVI4ODxxYU6=
U2OS M{LXVmZ2dmO2aX;uJIF{e2G7 NHH1VXZKdmirYnn0bY9vKG:oIFrBT|EwXFmNMjDpckBKTk5vYXzwbIFDOi2rbnT1Z4VlKGi3bXHuJHUzV1NiY3XscJMh[XO|ZYPz[YQh[XNicGPURXQyNCB;MD60N|bPxE1w MomxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NkmyO|AoRjJ3M{[5NlcxRC:jPh?=
HeLa MnjRSpVv[3Srb36gZZN{[Xl? NF3YO5BKdmirYnn0bY9vKG:oIFrBT|EwUkGNMjDpckBQW01vaX7keYNm\CCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IGPURXQyKHKncH;yeIVzNCB;MT6wOFXPxE1w NYLoPGFVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOlkzPzBpPkK1N|Y6OjdyPD;hQi=>
THP1 M1PyXWZ2dmO2aX;uJIF{e2G7 NIHpdXRKdmirYnn0bY9vKG:oIFrBT|EwUkGNMjDpckBKTk6pYX3tZU1qdmS3Y3XkJIh2dWGwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMheFOWQWSxMEA:Oy5|NkVOwG0v M4fH[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{[5NlcxLz5{NUO2PVI4ODxxYU6=
TF1 NUPmRod5TnWwY4Tpc44h[XO|YYm= M3;2U2lvcGmkaYTpc44hd2ZiSlHLNkBqdiCLTEOtbY5lfWOnZDDoeY1idiCWRkGgZ4VtdHNiYYPz[ZN{\WRiYYOgdHNVSVR3LDC9N{42OjUQvF2u NFLPbWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO2PVI4OCd-MkWzOlkzPzB:L3G+
BaF3 M2raRWZ2dmO2aX;uJIF{e2G7 MmfuTY5pcWKrdHnvckBw\iCMQVuyJIlvKEmOMz3pcoR2[2WmIHj1cYFvKEKjRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCycn;sbYZmemG2aX;uMEA:PC53NEdOwG0v MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN4OUK3NEc,OjV|NkmyO|A9N2F-
SJ-GBM2 Mn3qdWhVWyCjc4PhfS=> M{S2b5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NWL3Nm9oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 M323SZFJXFNiYYPzZZk> M2LaS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NHHzXmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MlT5dWhVWyCjc4PhfS=> MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NX3XWW9zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M1i3eZFJXFNiYYPzZZk> NH;GfnVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= M4OydlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NGjOfIVyUFSVIHHzd4F6 NEfFNJZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NE\FTFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MWHxTHRUKGG|c3H5 NUTwfXBTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 NYrRUGRReUiWUzDhd5NigQ>? M2W0d5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NVLsbWdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 MUHxTHRUKGG|c3H5 NHTXcJFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= NIfUO|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD M{m5TJFJXFNiYYPzZZk> MmS4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NWrNeXRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NWTYdVNjeUiWUzDhd5NigQ>? MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? M13GblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 28191885
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]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Rat CIA model and mouse CIA model
  • Dosages: 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
  • Administration: p.o.

Solubility (25°C)

In vitro

DMSO 85 mg/mL
(199.76 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 425.50
Formula

C21H23N5O3S

CAS No. 1206161-97-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03417778 Completed Drug: Filgotinib Rheumatoid Arthritis Gilead Sciences|Galapagos NV April 3 2018 Phase 1
NCT03117270 Completed Drug: filgotinib|Drug: Placebo Oral Tablet Ankylosing Spondylitis Galapagos NV March 7 2017 Phase 2
NCT03101670 Completed Drug: filgotinib|Drug: Placebo Oral Tablet Psoriatic Arthritis Galapagos NV March 9 2017 Phase 2
NCT02914600 Enrolling by invitation Drug: Filgotinib|Drug: Placebo Crohn''s Disease Gilead Sciences|Galapagos NV March 17 2017 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Could you recommemd a vehicle for oral gavage for S7605?

Answer:
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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