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CP-690550 (Tofacitinib) Citrate JAK remmer

Cat.nr.S5001

Tofacitinibcitraat (CP-690550, Tasocitinib) is een nieuwe JAK-remmer met IC50 van respectievelijk 1 nM, 20 nM en 112 nM tegen JAK3, JAK2 en JAK1. Het heeft ook Anti-infection activiteit.

CP-690550 (Tofacitinib) Citrate JAK remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 504.49

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	EGFR STAT Pim
Overig JAK Inhibitoren	BMS-986165 (Deucravacitinib) AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) Pacritinib TG101209 Cerdulatinib (PRT062070) hydrochloride

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK3 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0004 μM.	23668484
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.0006 μM.	22087750
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK1 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM.	23668484
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK2 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM.	23668484
Sf9	Function assay			Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA, IC50 = 0.001 μM.	14593182
Sf9	Function assay			Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.001 μM.	21105711
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.003 μM.	22087750
Sf9	Function assay			Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.0033 μM.	21105711
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.004 μM.	22087750
SF21	Function assay		10 mins	Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis, IC50 = 0.004 μM.	23541670
insect cells	Function assay			Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP, IC50 = 0.0061 μM.	21155605
insect cells	Function assay			Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP, IC50 = 0.008 μM.	21155605
T-cells	Function assay		72 hrs	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.011 μM.	14593182
insect	Function assay			Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP, IC50 = 0.012 μM.	21155605
MO7	Function assay			Inhibition of Jak3-mediated IL15-induced Stat5 phosphorylation in human MO7 cells by cell-based assay, IC50 = 0.024 μM.	21155605
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.026 μM.	22087750
T-cells	Function assay			Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation, IC50 = 0.028 μM.	23540648
PBMC	Function assay			Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry, IC50 = 0.039 μM.	26927423
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood, EC50 = 0.043 μM.	23659214
TF1	Function assay			Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay, INH = 0.045 μM.	26372653
CTLL	Function assay			Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay, IC50 = 0.048 μM.	21155605
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.052 μM.	22087750
TF1	Function assay			Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation, EC50 = 0.053 μM.	22591402
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins, EC50 = 0.053 μM.	22698084
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.053 μM.	23659214
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.054 μM.	22087750
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in monkey T cells by mixed lymphocyte reaction method, IC50 = 0.057 μM.	14593182
CD34+	Function assay			Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation, IC50 = 0.071 μM.	26927423
TF1	Function assay			Inhibition of IL4-induced proliferation of TF1 cells, IC50 = 0.08 μM.	16934457
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.087 μM.	14593182
TF1	Function assay		20 mins	Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins, EC50 = 0.093 μM.	22698084
TF1	Function assay		20 mins	Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.093 μM.	23659214
PBMC	Function assay			Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion, IC50 = 0.095 μM.	26927423
TF1	Function assay		2 hrs	Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis, IC50 = 0.095 μM.	27130359
TF1	Function assay			Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay, IC50 = 0.107 μM.	29156136
Sf9	Function assay			Inhibition of GST-tagged human JAK1 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.11 μM.	21105711
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.115 μM.	14593182
ME180	Function assay			Inhibition of JAK1 in IL6-stimulated human ME180 cells expressing stably integrated beta-lactamase reporter gene under control of sis-inducible element by fluorescence assay, IC50 = 0.124 μM.	29156136
CTLL-2	Antiproliferative assay		72 hrs	Antiproliferative activity against IL-2-stimulated mouse CTLL-2 cells expressing JAK1/JAK3 after 72 hrs by alamar blue assay, IC50 = 0.132 μM.	19762238
HT2	Function assay			Inhibition of JAK3 in mouse HT2 cells assessed as suppression of cell growth, IC50 = 0.156 μM.	27771180
DND/L12	Function assay		30 mins	Inhibition of JAK3 in human DND/L12 cells after 30 mins by luciferase assay in presence of human serum albumin, IC90 = 0.16 μM.	14593182
T-cells	Function assay			Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation, IC50 = 0.17 μM.	23540648
insect cells	Function assay			Inhibition of GST-tagged Tyk2 expressed in insect cells using 35 uM ATP, IC50 = 0.176 μM.	21155605
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.265 μM.	22087750
TF1	Function assay			Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth, IC50 = 0.2751 μM.	27771180
CD34+	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, IC50 = 0.302 μM.	24417533
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	14593182
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	21105711
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	19762238
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	30460842
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	23659214
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	16934457
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	26372653
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	22087750
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	30139575
A2780	Function assay			Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells	27771180
YT	Function assay	30 ng/ml		Inhibition of IL2-induced JAK3 phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
YT	Function assay	30 ng/ml		Inhibition of IL2-induced STAT5A phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
YT	Function assay	30 ng/ml		Inhibition of IL2-induced STAT5B phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
NK	Immunosuppressive assay	1 to 5 mg/kg	4 weeks	Immunosuppressive activity in naive cynomolgus monkey assessed as effect on CD3-CD16+ NK cells at 1 to 5 mg/kg, po for 4 weeks	14593182
T-cells	Function assay	5 to 500 nM	1 hr	Inhibition of IL2-induced Stat5 phosphorylation in human CD4+ T cells at 5 to 500 nM after 1 hr by Western blot	19053756
SUM149PT	Function assay	3 uM	16 hrs	Induction of PTPN6 in human SUM149PT cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate	24978112
Hs578T	Function assay	3 uM	16 hrs	Induction of PTPN6 in human Hs578T cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate	24978112
T-cells	Function assay	50 to 300 nM	1 hr	Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL4-stimulated STAT6 phosphorylation at 50 to 300 nM preincubated for 1 hr followed by IL-4 stimulation measured after 30 mins by immunoblot analysis	29852068
T-cells	Function assay	50 to 300 nM	1 hr	Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL2-stimulated STAT5 phosphorylation at Tyr-695 residue at 50 to 300 nM preincubated for 1 hr followed by IL-2 stimulation measured after 30 mins by immunoblot analysis	29852068
T-cells	Function assay	>300 nM	1 hr	Inhibition of JAK1/JAK2/TYK2 in human CD4 positive T cells assessed as inhibition of IL6-stimulated STAT3 phosphorylation at >300 nM preincubated for 1 hr followed by IL-6 stimulation measured after 30 mins by immunoblot analysis	29852068
TALL-1	Function assay	1 uM	3 hrs	Inhibition of JAK3 in human TALL-1 cells assessed as inhibition of IL-2 induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by IL-2 induction measured after 30 mins by immunoblotting	26258521
BA/F3	Function assay	300 nM	3 hrs	Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells assessed as reduction of STAT5 phosphorylation at 300 nM after 3 hrs by immunoblotting analysis	26258521
OCL-AML5	Function assay	1 uM	3 hrs	Inhibition of JAK2 in human OCL-AML5 cells assessed as inhibition of GM-CSF induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by GM-CSF induction measured after 30 mins by immunoblotting	26258521
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	26258521
BA/F3	Function assay	1 uM	3 hrs	Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells at 1 uM preincubated for 3 hrs followed by pulldown with streptavidin beads by immunoblotting analysis	26258521
Huh7	Function assay	10 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 10 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting	26231159
Huh7	Function assay	10 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of basal level STAT3 phosphorylation at 10 uM after 30 mins by immunoblotting	26231159
Huh7	Function assay	1 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 1 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting	26231159
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	504.49	Formule	C₁₆H₂₀N₆O.C₆H₈O₇	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	540737-29-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	Tasocitinib Citrate,CP-690550			Smiles	CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (198.21 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
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Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.500mg/ml (4.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	JAK3 (Cell-free assay) 1 nM JAK2 (Cell-free assay) 20 nM
In vitro	Tofacitinibcitraat remt IL-2-gemedieerde proliferatie van menselijke T-celblasten en IL-15-geïnduceerde CD69-expressie met een IC50 van respectievelijk 11 nM en 48 nM. Tofacitinibcitraat voorkomt gemengde lymfocytenreactie met een IC50 van 87 nM. Behandeling van muizenfactorafhankelijke cel Patersen-erytropoëtinerceptor (FDCP-EpoR) cellen die humaan wildtype of V617F JAK2 bevatten met tofacitinibcitraat leidt tot preventie van celproliferatie met een IC50 van respectievelijk 2,1 µM en 0,25 µM. Tofacitinibcitraat remt interleukine-6-geïnduceerde fosforylering van STAT1 en STAT3 met een IC50 van respectievelijk 23 nM en 77 nM. Bovendien genereert tofacitinibcitraat een significant pro-apoptotisch effect op muizen FDCP-EpoR-cellen die JAK2V^V617F dragen, terwijl een kleiner effect wordt waargenomen voor cellen die wildtype JAK2 dragen. Deze activiteit is gekoppeld aan de remming van fosforylering van de belangrijkste JAK2^V617F-afhankelijke stroomafwaartse signaaltransductoren en -activatoren van transcriptie (STAT)3, STAT5 en v-akt murine thymoma virale oncogenhomoloog (AKT). Bovendien voorkomt tofacitinibcitraat IL-15-geïnduceerde CD69-expressie in menselijke en cynomolgusapen NK- en CD8+ T-cellen in vitro.
Kinase Assay	Enzymtests
Kinase Assay	De JAK1, JAK2 en JAK3 kinase assays maken gebruik van een eiwit dat tot expressie wordt gebracht in baculovirus-geïnfecteerde SF9 cellen (een fusie-eiwit van GST en het katalytische domein van humaan JAK enzym) gezuiverd door affiniteitschromatografie op glutathion-Sepharose. Het substraat voor de reactie is polyglutaminezuur-tyrosine [PGT (4:1)], gecoat op Nunc Maxi Sorp platen bij 100 μg/mL overnacht bij 37 °C. De platen worden driemaal gewassen en JAK enzym wordt toegevoegd aan de putjes, die 100 μL kinasebuffer (50 mM HEPES, pH 7,3, 125 mM NaCl, 24 mM MgCl₂) + ATP + 1 mM natriumorthovanadaat bevatten. Voor CP-690550 (Tofacitinib) Citrate wordt het ook in verschillende doseringen toegevoegd voor de kinase assay. Na incubatie bij kamertemperatuur gedurende 30 min worden de platen driemaal gewassen. Het niveau van gefosforyleerd tyrosine in een gegeven putje wordt bepaald door een standaard ELISA-assay met behulp van een anti-fosfotyrosine antilichaam.
In vivo	Tofacitinibcitraat verminderde een vertraagde type overgevoeligheidsreactie en verlengde de overleving van cardiale allograften in muismodellen. Bovendien resulteert Tofacitinibcitraatbehandeling van ex-vivo geëxpandeerde erytroïde voorlopercellen van JAK2^V617F-positieve PV-patiënten in specifieke, antiproliferatieve (IC50 = 0,2 μM) en pro-apoptotische activiteit. Daarentegen zijn geëxpandeerde voorlopercellen van gezonde controles minder gevoelig voor Tofacitinibcitraat in proliferatie (IC50 > 1,0 μM) en apoptoseassays. Gedurende 2 weken Tofacitinibcitraatdosering van 10 en 30 mg/kg/d wordt een significante, tijdsafhankelijke afname van het aantal NK-cellen ten opzichte van vehikelbehandeling waargenomen. Het aantal effector-geheugen CD8+-cellen in de Tofacitinibcitraatbehandelde groep is 55% lager dan dat waargenomen bij dieren behandeld met vehikel.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/21105711/ [2] https://pubmed.ncbi.nlm.nih.gov/18482053/ [3] https://pubmed.ncbi.nlm.nih.gov/15371489/ [4] https://pubmed.ncbi.nlm.nih.gov/14593182/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	JAK3 / p-JAK3 / STAT3 LMP1 / EBNA1 / BZLF1 JAK3 / STAT5 / p-STAT5		26082451
Growth inhibition assay	Cell number		27732937

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT06202560	Enrolling by invitation	Frontal Fibrosing Alopecia\|Lichen Planopilaris	Institute of Dermatology Thailand	November 29 2023	Not Applicable
NCT05487703	Completed	Arthritis Rheumatoid	Pfizer	November 14 2022	--
NCT05082428	Completed	Ulcerative Colitis	Pfizer	May 30 2022	--
NCT05728008	Completed	Ulcerative Colitis	IRCCS San Raffaele	April 5 2022	--
NCT04768504	Recruiting	Immune-Mediated Colitis	Khashayar Esfahani\|Sir Mortimer B. Davis - Jewish General Hospital	March 22 2022	Phase 2

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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Veelgestelde vragen

Vraag 1:
What is the difference between the two products (S5001, S2789)?

Antwoord:
Tofacitinib (S2789) is the base form of this compound. The biological activity of these two compounds is the same. However, S5001 is better than S2789 for oral gavage.

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