pour la recherche uniquement
Réf. CatalogueS5001
| Cibles apparentées | EGFR STAT Pim |
|---|---|
| Autre JAK Inhibiteurs | BMS-986165 (Deucravacitinib) AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) Pacritinib TG101209 Cerdulatinib (PRT062070) hydrochloride |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | |
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| Poids moléculaire | 504.49 | Formule | C16H20N6O.C6H8O7 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 540737-29-9 | Télécharger le SDF | Stockage des solutions mères |
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| Synonymes | 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 | ||
|
In vitro |
DMSO
: 100 mg/mL
(198.21 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
JAK3
(Cell-free assay) 1 nM
JAK2
(Cell-free assay) 20 nM
|
|---|---|
| In vitro |
Le citrate de tofacitinib inhibe la prolifération des cellules T humaines médiée par l'IL-2 et l'expression du CD69 induite par l'IL-15 avec des IC50 de 11 nM et 48 nM, respectivement. Le citrate de tofacitinib prévient la réaction lymphocytaire mixte avec une IC50 de 87 nM. Le traitement des cellules Patersen-récepteur de l'érythropoïétine (FDCP-EpoR) murines dépendantes d'un facteur, abritant le JAK2 humain de type sauvage ou V617F, par le citrate de tofacitinib conduit à la prévention de la prolifération cellulaire avec des IC50 de 2,1 µM et 0,25 µM, respectivement. Le citrate de tofacitinib inhibe la phosphorylation de STAT1 et STAT3 induite par l'interleukine-6 avec des IC50 de 23 nM et 77 nM, respectivement. De plus, le citrate de tofacitinib génère un effet pro-apoptotique significatif sur les cellules FDCP-EpoR murines portant JAK2VV617F, tandis qu'un effet moindre est observé pour les cellules portant le JAK2 de type sauvage. Cette activité est couplée à l'inhibition de la phosphorylation des effecteurs de signalisation en aval clés dépendants de JAK2V617F, le transducteur de signal et activateur de transcription (STAT)3, STAT5, et l'homologue de l'oncogène viral du thymome murin v-akt (AKT). De plus, le citrate de tofacitinib prévient l'expression du CD69 induite par l'IL-15 dans les cellules NK et les cellules T CD8+ humaines et de singe cynomolgus in vitro.
|
| Essai kinase |
Dosages enzymatiques
|
|
Les tests kinases JAK1, JAK2 et JAK3 utilisent une protéine exprimée dans des cellules SF9 infectées par le baculovirus (une protéine de fusion du GST et du domaine catalytique de l'enzyme JAK humaine) purifiée par chromatographie d'affinité sur glutathion-Sépharose. Le substrat de la réaction est l'acide polyglutamique-tyrosine [PGT (4:1)], enrobé sur des plaques Nunc Maxi Sorp à 100 μg/mL pendant la nuit à 37 °C. Les plaques sont lavées trois fois, et l'enzyme JAK est ajoutée aux puits, qui contenaient 100 μL de tampon de kinase (50 mM HEPES, pH 7,3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM d'orthovanadate de sodium. Pour CP-690550 (Tofacitinib) Citrate, il est également ajouté pour le test kinase à différentes doses. Après incubation à température ambiante pendant 30 min, les plaques sont lavées trois fois. Le niveau de tyrosine phosphorylée dans un puits donné est déterminé par un test ELISA standard utilisant un anticorps anti-phosphotyrosine.
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| In vivo |
Le citrate de Tofacitinib diminue une réponse d'hypersensibilité de type retardé et prolonge la survie d'allogreffes cardiaques dans des modèles murins. De plus, le traitement par citrate de Tofacitinib de progéniteurs érythroïdes ex-vivo expansés de patients atteints de PV positifs pour JAK2V617F entraîne une activité spécifique antiproliférative (IC50 = 0,2 μM) et pro-apoptotique. En revanche, les progéniteurs expansés de contrôles sains sont moins sensibles au citrate de Tofacitinib en termes de prolifération (IC50 > 1,0 μM) et d'essais d'apoptose. Au cours de 2 semaines d'administration de citrate de Tofacitinib à des doses de 10 et 30 mg/kg/j, une diminution significative et dépendante du temps du nombre de cellules NK par rapport au traitement avec le véhicule est observée. Le nombre de cellules CD8+ à mémoire effectrice dans le groupe traité par citrate de Tofacitinib est 55% inférieur à celui observé chez les animaux traités avec le véhicule.
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Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | JAK3 / p-JAK3 / STAT3 LMP1 / EBNA1 / BZLF1 JAK3 / STAT5 / p-STAT5 |
|
26082451 |
| Growth inhibition assay | Cell number |
|
27732937 |
(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| 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 |
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Question 1:
What is the difference between the two products (S5001, S2789)?
Réponse :
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.