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Tofacitinib

(Synonyms: Tasocitinib; CP-690550)

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Tofacitinib is an orally available JAK3/2/1 inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively.

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Reinheit: 99.94%
CAS. Nr.: 477600-75-2
Formel: C₁₆H₂₀N₆O
Molecular Weight:312.37

Speicherung:

4°C, protect from light.

In solvent -80°C, 2 years , -20°C, 1 year

Tofacitinib Chemical Structure

CAS. Nr.: 477600-75-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (100)
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- In Vitro
- In Vivo
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Biologische Aktivität

Beschreibung

Tofacitinib is an orally available JAK3/2/1 inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively.

IC₅₀ & Target^[1]

JAK3

1 nM (IC₅₀)

JAK2

20 nM (IC₅₀)

JAK1

112 nM (IC₅₀)

Rock-II

3400 nM (IC₅₀)

Lck

3870 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.1 μM Compound: Tofacitinib	Antiproliferative activity against human A549 cells incubated for 24 to 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells incubated for 24 to 48 hrs by CCK8 assay	[PMID: 33234343]
BaF3	IC₅₀	1574 nM Compound: CP-690550	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
BaF3	IC₅₀	570 nM Compound: CP-690550	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
BaF3	IC₅₀	0.026 μM Compound: 20, CP-690550	Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay	[PMID: 22087750]
BaF3	IC₅₀	0.054 μM Compound: 20, CP-690550	Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay	[PMID: 22087750]
BaF3	IC₅₀	0.265 μM Compound: 20, CP-690550	Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay	[PMID: 22087750]
BaF3	IC₅₀	1.2 μM Compound: 20, CP-690550	Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay	[PMID: 22087750]
BaF3	IC₅₀	177.3 nM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	4154.3 nM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	516.5 nM Compound: 2	Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	IC₅₀	8884.6 nM Compound: 2	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]
BaF3	GI₅₀	0.044 μM Compound: 1	Growth inhibition of mouse BaF3 cells harboring JAK1 measured after 72 hrs by CCK-8 assay Growth inhibition of mouse BaF3 cells harboring JAK1 measured after 72 hrs by CCK-8 assay	[PMID: 38031930]
BaF3	GI₅₀	0.302 μM Compound: 1	Growth inhibition of mouse BaF3 cells harboring TYK2 measured after 72 hrs by CCK-8 assay Growth inhibition of mouse BaF3 cells harboring TYK2 measured after 72 hrs by CCK-8 assay	[PMID: 38031930]
BaF3	GI₅₀	0.46 μM Compound: 1	Growth inhibition of mouse BaF3 cells harboring JAK3 measured after 72 hrs by CCK-8 assay Growth inhibition of mouse BaF3 cells harboring JAK3 measured after 72 hrs by CCK-8 assay	[PMID: 38031930]
BaF3	GI₅₀	1.382 μM Compound: 1	Growth inhibition of mouse BaF3 cells harboring JAK2 measured after 72 hrs by CCK-8 assay Growth inhibition of mouse BaF3 cells harboring JAK2 measured after 72 hrs by CCK-8 assay	[PMID: 38031930]
CTLL	IC₅₀	48 nM Compound: 2, CP-690550	Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay	[PMID: 21155605]
HEL	IC₅₀	4724 nM Compound: Tofacitinib	Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr	[PMID: 27771180]
HEL	IC₅₀	5.2 μM Compound: Tofacitinib	Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant measured after 48 hrs by CellTiter-Glo assay	[PMID: 30846405]
HEL	IC₅₀	4724 nM Compound: 1	Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation Inhibition of JAK2 V617F mutant in human HEL cells assessed as reduction in cell proliferation	[PMID: 30926315]
HEL	IC₅₀	3.83 μM Compound: Tofacitinib	Cytotoxicity against HEL cells assessed as inhibition of cell growth Cytotoxicity against HEL cells assessed as inhibition of cell growth	[PMID: 36805946]
HeLa	IC₅₀	0.04 μM Compound: Tofacitinib	Antiproliferative activity against human Hela cells incubated for 24 to 48 hrs by CCK8 assay Antiproliferative activity against human Hela cells incubated for 24 to 48 hrs by CCK8 assay	[PMID: 33234343]
HepG2	IC₅₀	0.11 μM Compound: Tofacitinib	Antiproliferative activity against human HepG2 cells incubated for 24 to 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells incubated for 24 to 48 hrs by CCK8 assay	[PMID: 33234343]
HFF	IC₅₀	>10000 nM Compound: CP-690550	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
HFF	IC₅₀	>10000 nM Compound: 1	Inhibition of HFF proliferation after 72 hrs by [3H]thymidine incorporation assay Inhibition of HFF proliferation after 72 hrs by [3H]thymidine incorporation assay	[PMID: 21105711]
Jurkat	IC₅₀	7840 nM Compound: CP-690550	Inhibition of anti-CD3/anti-CD28-induced IL2 production in human Jurkat cells after 24 hrs by scintillation counting Inhibition of anti-CD3/anti-CD28-induced IL2 production in human Jurkat cells after 24 hrs by scintillation counting	[PMID: 14593182]
Jurkat	IC₅₀	>5000 nM Compound: 2, CP-690550	Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence	[PMID: 21155605]
MCF7	IC₅₀	>100 μM Compound: Tofacitinib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 32682202]
MGC-803	IC₅₀	>100 μM Compound: Tofacitinib	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 32682202]
NCI-H1975	IC₅₀	>100 μM Compound: Tofacitinib	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 32682202]
PBMC	IC₅₀	39 nM Compound: Tofacitinib	Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry	[PMID: 26927423]
PBMC	IC₅₀	95 nM Compound: Tofacitinib	Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion	[PMID: 26927423]
PBMC	CC₅₀	>100 μM Compound: 31	Cytotoxicity against human PBMC Cytotoxicity against human PBMC	[PMID: 33539089]
PC-9	IC₅₀	>100 μM Compound: Tofacitinib	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 32682202]
Sf21	IC₅₀	0.004 μM Compound: CP690, 550	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 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	[PMID: 23541670]
Sf21	IC₅₀	4.1 nM Compound: 2	Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay	[PMID: 27555284]
Sf21	IC₅₀	0.0012 μM Compound: 1; CP-690,550	Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method	[PMID: 32511913]
Sf9	IC₅₀	1 nM Compound: CP-690550	Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA	[PMID: 14593182]
Sf9	IC₅₀	110 nM Compound: 18m	Inhibition of GST-tagged human JAK1 catalytic domain expressed in Sf9 cells by ELISA Inhibition of GST-tagged human JAK1 catalytic domain expressed in Sf9 cells by ELISA	[PMID: 21105711]
Sf9	IC₅₀	0.003 μM Compound: 20, CP-690550	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 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	[PMID: 22087750]
Sf9	IC₅₀	0.004 μM Compound: 20, CP-690550	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 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	[PMID: 22087750]
Sf9	IC₅₀	0.052 μM Compound: 20, CP-690550	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 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	[PMID: 22087750]
Sf9	IC₅₀	0.0006 μM Compound: 20, CP-690550	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 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	[PMID: 22087750]
Sf9	IC₅₀	0.6 nM Compound: 20, CP-690550	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 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	[PMID: 22087750]
Sf9	IC₅₀	0.0011 μM Compound: 1; CP-690,550	Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method	[PMID: 32511913]
Splenocyte	IC₅₀	23 nM Compound: 1	Immunosuppressive activity in Lewis rat splenocytes assessed as inhibition of concanavalin A-induced IL-2 receptor expression incubated for 3 days by alamarBlue assay Immunosuppressive activity in Lewis rat splenocytes assessed as inhibition of concanavalin A-induced IL-2 receptor expression incubated for 3 days by alamarBlue assay	[PMID: 28789911]
T-cell	IC₅₀	11 nM Compound: CP-690550	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	115 nM Compound: CP-690550	Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	57 nM Compound: CP-690550	Inhibition of allogenic cells-stimulated proliferation in monkey T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in monkey T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	87 nM Compound: CP-690550	Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	185 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK2 in mouse whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK2 in mouse whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	187 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in rat whole blood assessed as reduction in IL-21-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in rat whole blood assessed as reduction in IL-21-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	25 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-21-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-21-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	28 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	367 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK2 in human whole blood assessed as reduction in IL-6-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-6 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK2 in human whole blood assessed as reduction in IL-6-induced STAT3 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-6 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	38 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-7-induced STAT5 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-7 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-7-induced STAT5 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-7 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	42 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in mouse whole blood assessed as reduction in IL-15-induced STAT5 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in mouse whole blood assessed as reduction in IL-15-induced STAT5 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	44 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IFN-alpha stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IFN-alpha stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	50 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-4-induced STAT6 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-4 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-4-induced STAT6 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-4 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	54 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK2 in human whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-6 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK2 in human whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD3+ T cells preincubated for 1 hr followed by IL-6 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	56 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-15-induced STAT5 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-15-induced STAT5 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	62 nM Compound: Chemical probe: CP-690,550	Inhibition of JAK1/JAK2 in rat whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis Inhibition of JAK1/JAK2 in rat whole blood assessed as reduction in IL-6-induced STAT1 phosphorylation in CD8+ T cells preincubated for 1 hr followed by IL-2 stimulation and measured after 8 to 20 mins by FACS analysis	[PMID: 20701804]
T-cell	IC₅₀	0.028 μM Compound: 1a	Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation	[PMID: 23540648]
T-cell	IC₅₀	0.17 μM Compound: 1a	Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation	[PMID: 23540648]
T-cell	IC₅₀	33 nM Compound: Tofacitinib	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-2-induced STAT5 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-2 addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	74 nM Compound: Tofacitinib	Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	740 nM Compound: Tofacitinib	Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	76 nM Compound: Tofacitinib	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFN-alpha-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IFN-alpha addition and measured after 20 mins by flow cytometry analysis	[PMID: 24006460]
T-cell	IC₅₀	23 nM Compound: 1, CP-690,550	Inhibition of JAK1/JAK3 in Lewis rat splenocytes assessed as reduction in IL2-induced T cell proliferation incubated for 3 days by alamar blue assay Inhibition of JAK1/JAK3 in Lewis rat splenocytes assessed as reduction in IL2-induced T cell proliferation incubated for 3 days by alamar blue assay	[PMID: 26059596]
T-cell	IC₅₀	2 nM Compound: Tofacitinib	Antiproliferative activity against rat T cells cultured with Concanavalin A for 24 hrs assessed inhibition of IL-2-stimulated cell proliferation after 72 hrs by MTS assay Antiproliferative activity against rat T cells cultured with Concanavalin A for 24 hrs assessed inhibition of IL-2-stimulated cell proliferation after 72 hrs by MTS assay	[PMID: 30853331]
T-cell	IC₅₀	16 nM Compound: 1	Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis	[PMID: 32120325]
T-cell	IC₅₀	0.016 μM Compound: 1; CP-690,550	Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method	[PMID: 32511913]
TF-1	IC₅₀	80 nM Compound: CP-690550	Inhibition of IL4-induced proliferation of TF1 cells Inhibition of IL4-induced proliferation of TF1 cells	[PMID: 16934457]
TF-1	IC₅₀	800 nM Compound: CP-690550	Inhibition of IL3-induced proliferation of TF1 cells Inhibition of IL3-induced proliferation of TF1 cells	[PMID: 16934457]
TF-1	IC₅₀	80 nM Compound: CP-690550	Inhibition of IL4-induced TF1 cell proliferation Inhibition of IL4-induced TF1 cell proliferation	[PMID: 17189692]
TF-1	IC₅₀	800 nM Compound: CP-690550	Inhibition of IL3-induced TF1 cell proliferation Inhibition of IL3-induced TF1 cell proliferation	[PMID: 17189692]
TF-1	EC₅₀	53 nM Compound: 1, CP-690550, Tofacitinib	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation	[PMID: 22591402]
TF-1	EC₅₀	53 nM Compound: 1, CP-690550	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 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	[PMID: 22698084]
TF-1	EC₅₀	93 nM Compound: 1, CP-690550	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 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	[PMID: 22698084]
TF-1	EC₅₀	43 nM Compound: 1, CP-690,550, Tofacitinib, Xeljanz	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 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	[PMID: 23659214]
TF-1	EC₅₀	53 nM Compound: 1, CP-690,550, Tofacitinib, Xeljanz	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 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	[PMID: 23659214]
TF-1	EC₅₀	93 nM Compound: 1, CP-690,550, Tofacitinib, Xeljanz	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 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	[PMID: 23659214]
TF-1	IC₅₀	0.095 μM Compound: Tofacitinib	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 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	[PMID: 27130359]
TF-1	IC₅₀	275.1 nM Compound: Tofacitinib	Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth	[PMID: 27771180]
TF-1	IC₅₀	2.6 μM Compound: Tofacitinib	Antiproliferative activity against JAK2 wild-type human TF1 cells measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against JAK2 wild-type human TF1 cells measured after 48 hrs by CellTiter-Glo assay	[PMID: 30846405]
TF-1	IC₅₀	275.1 nM Compound: 1	Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation Inhibition of JAK2 in human TF-1 cells assessed as reduction in GM-CSF-induced cell proliferation	[PMID: 30926315]
TF-1	IC₅₀	0.12 μM Compound: 20	Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay	[PMID: 32462873]
THP-1	IC₅₀	0.9 μM Compound: Tofacitinib	Cytotoxicity against IL-4 induced JAK1/3 activated human THP1 cells preincubated for 1 hr followed by IL-4 induction and measured after 1 hr by CellTiter-Glo assay Cytotoxicity against IL-4 induced JAK1/3 activated human THP1 cells preincubated for 1 hr followed by IL-4 induction and measured after 1 hr by CellTiter-Glo assay	[PMID: 30846405]
THP1-Dual	IC₅₀	24.8 nM Compound: Tofacitinib	Inhibition of LPS induced ISG activation in human THP1-Dual cells pretreated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs Inhibition of LPS induced ISG activation in human THP1-Dual cells pretreated with LPS-B5 for 3 hrs followed by compound addition incubated for 24 hrs	[PMID: 36053746]
U-251	IC₅₀	0.33 μM Compound: Tofacitinib	Antiproliferative activity against human U-251 cells incubated for 24 to 48 hrs by CCK8 assay Antiproliferative activity against human U-251 cells incubated for 24 to 48 hrs by CCK8 assay	[PMID: 33234343]
U-937	IC₅₀	122.4 nM Compound: 2	Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35860875]

In Vitro

Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (K_d). The report includes additional binding for Tofacitinib at Camk1 (K_d of 5,000 nM), DCamkL3 (K_d of 4.5 nM), Mst2 (K_d of 4,300 nM), Pkn1 (K_d of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (K_d of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (K_d of 1,200 nM), Snark (K_d of 420 nM), Tnk1 (K_d of 640 nM) and Tyk2 (K_d of 620 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Animals that are treated with Tofacitinib show a significantly lower production of anti-drug antibodies (ADAs) compare with PEG-treated control mice (for five weeks after initial immunization, p<0.01, n=8). Moreover ADAs become detectable earliest on day 28. A difference of 1000- to 200-fold in titers to SS1P is apparent from days 21 through 35, respectively. Compare to SS1P, mice injected with keyhole limpet hemocyanin (KLH) generate a more rapid antibody response. Yet, the administration of Tofacitinib reduces anti-KLH titers compare to controls (p<0.05 on day 21, p<0.01 on day 28, respectively, n=5). Reductions in titers ranged from 5000- to 250-fold from days 21 through 28, respectively^[2]. Based on previous dose-response studies, a daily dose of Tofacitinib of 6.2 mg/kg is selected to provide 80% inhibition of hind paw volume and plasma exposure capable of suppressing the JAK1 and JAK3 signaling pathways for >4 hours^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 477600-75-2
Appearance Solid
Molecular Weight 312.37
Formel C₁₆H₂₀N₆O
Color Off-white to light yellow
SMILES

O=C(CC#N)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C)[C@H](C)CC1
Synonyms

Tasocitinib; CP-690550
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, protect from light

In solvent	-80°C	2 years
	-20°C	1 year

Publications (100)

All IPWBFlow CytometryCell Imaging/Staining

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Journal Impact Factor

Nature

Microbial metabolite drives ageing-related clonal haematopoiesis via ALPK1. [Abstract]

2025 Jun;642(8066):201-211. PMID: 40269158
Adv Mater

3D Bioprinted Human Synovium-Cartilage Models Mimic Rheumatoid Arthritis Microenvironment and Recapitulate In Vivo Therapeutic Responses. [Abstract]

2025 Dec 12:e13952. PMID: 41388589
Ann Rheum Dis

Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]

2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174
Ann Rheum Dis

Positive feedback loop PU.1-IL9 in Th9 promotes rheumatoid arthritis development. [Abstract]

2024 Aug 20:ard-2024-226067. PMID: 39164066

Tofacitinib purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]

Western blot analysis was performed to detect PU.1 expression in Jurkat and EL4 cells treated with recombinant IL-9 and the JAK inhibitor tofacitinib (10 μM, 48 h).

Tofacitinib purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]

Western blot analysis was performed to detect the IL-9 effect on the JAK1/STAT3 pathway in RA-Th9 cells. The cell treated with tofacitinib (10 μM, 48 h), stattic (2.5 μM, 48 h).

Tofacitinib purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]

Flow cytometry was used to detect the JAK inhibitor tofacitinib (10 μM, 48 h) effect, STAT3 inhibitor stattics (2.5 μM, 48 h), and PU.1 inhibitor DB2313 on the release of IL-9 from Th9 cells.

Tofacitinib purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]

Flow cytometry was used to detect IL-9 and JAK inhibitor tofacitinib (10 μM, 48 h) effect, STAT3 inhibitor stattics (2.5 μM, 48 h) effect on TNF-α-induced apoptosis in Th9 cells.

Tofacitinib purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]

Assess the effects of tofacitinib (10 μM, 48 h), stattics (2.5 μM, 48 h), and IL-9mAb on the cell migration of RA-FLS after treatment with the supernatant from RA-Th9 cells.
Ann Rheum Dis

Immune response to dermatomyositis-specific autoantigen, transcriptional intermediary factor 1γ can result in experimental myositis. [Abstract]

2021 Sep;80(9):1201-1208. PMID: 33811031
Nat Commun

All-trans retinoic acid destabilizes ADAR1 protein through retinoylation-mediated USP7 dissociation and improves immunotherapy in pancreatic cancer. [Abstract]

2026 May 11. PMID: 42115161
Nat Commun

A loss-of-function human ADAR variant activates innate immune response and promotes bowel inflammation. [Abstract]

2025 Sep 29;16(1):8560. PMID: 41022715
Nat Commun

Priming with LSD1 inhibitors promotes the persistence and antitumor effect of adoptively transferred T cells. [Abstract]

2024 May 21;15(1):4327. PMID: 38773088
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

MAM-STAT3-Driven Mitochondrial Ca+2 Upregulation Contributes to Immunosenescence in Type A Mandibuloacral Dysplasia Patients. [Abstract]

2024 Dec 11:e2407398. PMID: 39661729
Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2024 Dec 5:e2410360. PMID: 39639496
Sci Adv

JAK/STAT signaling pathway affects CCR5 expression in human CD4+ T cells. [Abstract]

2024 Mar 22;10(12):eadl0368. PMID: 38507500
J Allergy Clin Immunol

Recapitulating primary immunodeficiencies with expanded potential stem cells: proof-of-concept with STAT1 gain-of-function. [Abstract]

2024 Apr;153(4):1125-1139. PMID: 38072195
Gut Microbes

The PTPN2 rs1893217 IBD risk allele increases susceptibility to AIEC invasion by a JAK-STAT-CEACAM6 axis. [Abstract]

2025 Dec;17(1):2526136. PMID: 40624731
MedComm (2020)

Loss of Adenosine Deaminase Acting on RNA 1 Induces Panoptosis and Immune Response in Ulcerative Colitis Gut Mucosa. [Abstract]

2025 Jun 6;6(6):e70212. PMID: 40487746
J Immunother Cancer

Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein. [Abstract]

2025 May 11;13(5):e010831. PMID: 40350206
J Immunother Cancer

JAK3 A573V and JAK3 M511I mutations in peripheral T-cell lymphoma mediating resistance to anti-PD-1 therapy through the STAT3/PD-L1 pathway. [Abstract]

2025 Apr 8;13(4):e010783. PMID: 40199606
Cell Rep Med

Chemical activation of mitochondrial ClpP to modulate energy metabolism of CD4+ T cell for inflammatory bowel diseases treatment. [Abstract]

2024 Nov 23:101840. PMID: 39626672
Proc Natl Acad Sci U S A

PARP12-mediated mono-ADP-ribosylation as a checkpoint for necroptosis and apoptosis. [Abstract]

2025 Jun 17;122(24):e2426660122. PMID: 40489618
Nano Res

2023 Apr 15.
Dev Cell

Tumor-intrinsic FDFT1 determines coordinated macrophage anti-tumor immunity. [Abstract]

2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405
Acta Pharmacol Sin

Tofacitinib prevents depressive-like behaviors through decreased hippocampal microgliosis and increased BDNF levels in both LPS-induced and CSDS-induced mice. [Abstract]

2025 Feb;46(2):353-365. PMID: 39349767
Phytomedicine

Astragali radix - Curcumae rhizoma herb pair enhances Sorafenib's efficacy by inducing ferroptosis and activates Th1 cell immune response synergistically against hepatocellular carcinoma. [Abstract]

2025 Sep 23:148:157326. PMID: 41016296
Phytomedicine

Anemoside B4 protects against chronic relapsing colitis in mice by modulating inflammatory response, colonic transcriptome and the gut microbiota. [Abstract]

2022 Nov:106:154416. PMID: 36037770
BMC Med

HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]

2021 Oct 15;19(1):247. PMID: 34649530
Free Radic Biol Med

Inhibiting Arachidonate-5-lipoxygenase expression ameliorates osteoarthritis progression by suppressing ferroptosis via the JAK2/STAT3 signaling pathway. [Abstract]

2026 Mar 16:246:334-349. PMID: 41581577
Free Radic Biol Med

Oxidative stress-induced IL-15 trans-presentation in keratinocytes contributes to CD8+ T cells activation via JAK-STAT pathway in vitiligo. [Abstract]

2019 Aug 1:139:80-91. PMID: 31078730
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Cell Mol Gastroenterol Hepatol

Tofacitinib Mitigates the Increased SARS-CoV-2 Infection Susceptibility Caused by an IBD Risk Variant in the PTPN2 Gene. [Abstract]

2025;19(5):101447. PMID: 39756517
Cell Mol Gastroenterol Hepatol

Tofacitinib-Induced Modulation of Intestinal Adaptive and Innate Immunity and Factors Driving Cellular and Systemic Pharmacokinetics. [Abstract]

2022;13(2):383-404. PMID: 34624526
Stem Cell Res Ther

LncRNA SNHG1 enhances cartilage regeneration by modulating chondrogenic differentiation and angiogenesis potentials of JBMMSCs via mitochondrial function regulation. [Abstract]

2024 Jun 18;15(1):177. PMID: 38886785
Cell Rep

IL-33/TGF-β/IL-4-induced bone marrow-derived DC9 subset promotes Th9 differentiation and allergic airway inflammation. [Abstract]

2026 Jun 4;45(6):117519. PMID: 42247295
Cell Rep

LTP expression mediated by autonomous activity of GluN2B-bound CaMKII. [Abstract]

2024 Oct 11;43(10):114866. PMID: 39395168
Cell Rep

The Natural Compound Notopterol Binds and Targets JAK2/3 to Ameliorate Inflammation and Arthritis. [Abstract]

2020 Sep 15;32(11):108158. PMID: 32937124
J Med Chem

Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof. [Abstract]

2021 Feb 25;64(4):2228-2241. PMID: 33570945
Phytother Res

(+)-Matairesinol, Derived From Olive Oil, Enhanced T-Cell Anti-Tumor Immune via JAK3-STAT1 Signal and Synergized With Anti-PD-1 Efficacy. [Abstract]

2026 Apr 27. PMID: 42037203
Phytother Res

Paeoniflorin-6'-o-benzene sulfonate (CP-25) improves vasculitis through inhibiting IL-17A/JAK/STAT3 signaling pathway in endothelial cells of HFD CIA rats. [Abstract]

2021 Feb;35(2):1033-1047. PMID: 33006176
Biochem Pharmacol

Glucocorticoid impairs angiogenesis-dependent osteogenesis by downregulating EphB4 in endothelial cells. [Abstract]

2025 Dec 2:244:117586. PMID: 41344513
Biochem Pharmacol

STING activation in macrophages by vanillic acid exhibits antineoplastic potential. [Abstract]

2023 Jul:213:115618. PMID: 37211172
Cell Prolif

FGF9 promotes mouse spermatogonial stem cell proliferation mediated by p38 MAPK signalling. [Abstract]

2021 Jan;54(1):e12933. PMID: 33107118
Biochem Pharmacol

Combined anti-fibrotic and anti-inflammatory properties of JAK-inhibitors on macrophages in vitro and in vivo: Perspectives for scleroderma-associated interstitial lung disease. [Abstract]

2020 Aug;178:114103. PMID: 32562787
J Ethnopharmacol

"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]

2026 Oct 28:369:121888. PMID: 42202911
Virulence

Immunosuppressants exert antiviral effects against influenza A(H1N1)pdm09 virus via inhibition on nucleic acid synthesis, mRNA splicing and protein stability. [Abstract]

2024 Dec;15(1):2301242. PMID: 38170681
Drug Des Devel Ther

Drug Interaction Potential of Berberine Hydrochloride When Co-Administered with Tofacitinib and Filgotinib in Rats. [Abstract]

2025 Jun 10:19:5043-5057. PMID: 40524804
CNS Neurosci Ther

Hypoxia Upregulates RIPK1 via the HIF-1α-JAK-STAT Pathway Leading to Astrocyte Necroptosis to Promote Cavitation After Spinal Cord Injury. [Abstract]

2026 May;32(5):e70895. PMID: 42109032
Inflammation

The Effect of JAK Inhibitor Tofacitinib on Chondrocyte Autophagy. [Abstract]

2023 Oct;46(5):1764-1776. PMID: 37310645
Respir Res

IL-37 protects against airway remodeling by reversing bronchial epithelial-mesenchymal transition via IL-24 signaling pathway in chronic asthma. [Abstract]

2022 Sep 13;23(1):244. PMID: 36100847
Pharmaceuticals (Basel)

Topical Delivery of Tofacitinib in Dermatology: The Promise of a Novel Therapeutic Class Using Biodegradable Dendritic Polyglycerol Sulfates. [Abstract]

2024 Jan 8;17(1):77. PMID: 38256910
Eur J Pharm Sci

Assessing the effects of tofacitinib on the gut microbiome in inflammatory bowel disease. [Abstract]

2026 Jan 1:216:107365. PMID: 41205933
Eur J Pharm Sci

Exploring the interactions of JAK inhibitor and S1P receptor modulator drugs with the human gut microbiome: Implications for colonic drug delivery and inflammatory bowel disease. [Abstract]

2024 Jul 4:106845. PMID: 38971433
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Inflamm Bowel Dis

The JAK-Inhibitor Tofacitinib Rescues Human Intestinal Epithelial Cells and Colonoids from Cytokine-Induced Barrier Dysfunction. [Abstract]

2020 Feb 11;26(3):407-422. PMID: 31751457
FASEB J

Targeting JAK2: Genetic and Pharmacological Inhibition Attenuates Immune-Mediated Liver Injury by Suppressing Proinflammatory Macrophage. [Abstract]

2026 Apr 30;40(8):e71804. PMID: 41984049
iScience

IFN-γ licenses normal and pathogenic ALPK1/TIFA pathway in human monocytes. [Abstract]

2024 Dec 10;28(1):111563. PMID: 39868044
iScience

Schlafen 11 expression in human acute leukemia cells with gain-of-function mutations in the interferon-JAK signaling pathway. [Abstract]

2021 Sep 25;24(10):103173. PMID: 34693224
J Biomed Mater Res A

A ROS-Responsive Hydrogel Microneedle System Co-Delivering Tofacitinib and Azelaic Acid for Enhanced Targeted Therapy of Rosacea. [Abstract]

2026 Feb;114(2):e70035. PMID: 41586451
J Biotechnol

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

2025 Mar:399:9-18. PMID: 39824361
Sci Rep

Identification of novel off targets of baricitinib and tofacitinib by machine learning with a focus on thrombosis and viral infection. [Abstract]

2022 May 12;12(1):7843. PMID: 35551258
Sci Rep

JAK/STAT inhibitor therapy partially rescues the lipodystrophic autoimmune phenotype in Clec16a KO mice. [Abstract]

2021 Apr 1;11(1):7372. PMID: 33795715
Food Sci Nutr

Chlorogenic Acid Ameliorate Lipopolysaccharide Induced Intestinal Acute Inflammatory Injury via Inhibiting Cytokines Production and Activating Intestinal Stem Cells. [Abstract]

2026 Mar 4;14(3):e71602. PMID: 41788896
J Pharmacol Exp Ther

Novel Inhaled Pan-JAK Inhibitor, LAS194046, Reduces Allergen-Induced Airway Inflammation, Late Asthmatic Response, and pSTAT Activation in Brown Norway Rats. [Abstract]

2019 Aug;370(2):137-147. PMID: 31085698
Mol Hum Reprod

Tofacitinib alters STAT3 signaling and leads to endometriosis lesion regression. [Abstract]

2021 Mar 24;27(4):gaab016. PMID: 33693775
Exp Cell Res

Down-regulation of A3AR signaling by IL-6-induced GRK2 activation contributes to Th17 cell differentiation. [Abstract]

2021 Feb 15;399(2):112482. PMID: 33434531
Food Chem Toxicol

Gallic and butyric acids modulated NLRP3 inflammasome markers in a co-culture model of intestinal inflammation. [Abstract]

2020 Dec;146:111835. PMID: 33130239
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
J Immunol

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. [Abstract]

2013 Oct 1;191(7):3568-77. PMID: 24006460
Mol Biol Rep

Janus kinase inhibitor Tofacitinib alleviated acute hepatitis induced by lipopolysaccharide/D-galactosamine in mice. [Abstract]

2023 Feb;50(2):1477-1485. PMID: 36507969
J Biochem Mol Toxicol

Lung-derived exosomes regulate the function of mesenchymal stem cells and alleviate phosgene-induced lung injury via miR-34c-3p. [Abstract]

2021 Sep;35(9):e22851. PMID: 34331784
Pulm Pharmacol Ther

Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. [Abstract]

2017 Apr:43:60-67. PMID: 28087469

Tofacitinib purchased from MedChemExpress. Usage Cited in: Pulm Pharmacol Ther. 2017 Apr:43:60-67. [Abstract]

Effect of Tofacitinib administered 1 h before LPS challenge. (A) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 30 min after LPS challenge. (B) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 4 h after LPS challenge.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

Application of a phenotypic drug discovery strategy to identify biological and chemical starting points for inhibition of TSLP production in lung epithelial cells. [Abstract]

2018 Jan 10;13(1):e0189247. PMID: 29320511
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Immunobiology

Dual-phase study of CD4+CXCR4+ T cells in Mycoplasma pneumoniae pneumonia: clinical correlations in children and therapeutic exploration with tofacitinib in mice. [Abstract]

2025 Nov;230(6):153136. PMID: 41192098
Arch Dermatol Res

Effect of propylene glycol on the skin penetration of drugs. [Abstract]

2020 Jul;312(5):337-352. PMID: 31786711
Planta Med

Active Components and Multi-target Mechanism of Tibetan Sinopodophyllum hexandrum Medicine Against Rheumatoid Arthritis Using a CFA-induced Arthritis Rat Model. [Abstract]

2025 Oct 20. PMID: 41115426
Int J Rheum Dis

MiR-1193 represses the proliferation and induces the apoptosis of interleukin-1β-treated fibroblast-like synoviocytes via targeting JAK3. [Abstract]

2020 Aug;23(8):1066-1075. PMID: 32597556
Biomed Chromatogr

Identification of the metabolites of tofacitinib in liver microsomes by liquid chromatography combined with high resolution mass spectrometry. [Abstract]

2021 Jun;35(6):e5081. PMID: 33522621
Iran J Immunol

JAK/STAT Signaling Pathway Mediates Anti-Tumor Immunity of CD8+ T Cells in Renal Cancer. [Abstract]

2024 Sep 25;21(3). PMID: 39319693
bioRxiv

2026 May 29.
bioRxiv

2026 May 5.
J Can Res Updates

2026.
bioRxiv

Multiplexed high-content imaging uncovers morphological diversity of lymphocyte activation and dysfunction. [Abstract]

2026 Feb 11:2026.02.10.704860. PMID: 41726991
Res Sq

2025 Sep 26.
SSRN

2025 Sep 3.
bioRxiv

2025 Aug 16.
Res Sq

2025 Apr 16.
bioRxiv

2025 February 21.
bioRxiv

All-trans retinoic acid-mediated ADAR1 degradation synergizes with PD-1 blockade to suppress pancreatic cancer. [Abstract]

2024 Oct 23:2024.10.20.619300. PMID: 39484589
medRxiv

The JAK inhibitor, Tofacitinib, Corrects the Overexpression of CEACAM6 and Limits Susceptibility to AIEC Caused by Reduced Activity of the IBD Associated Gene, PTPN2. [Abstract]

2024 Sep 28:2024.09.26.24314341. PMID: 39399045
Research Square Preprint

2024 Apr 19.
bioRxiv

2024 Jan 24.
Chemrxiv

2023 Aug 3.
Research Square Print

2023 Mar 14.
Research Square Print

January 9th, 2023.
Patent

US20220274992A1.
Research Square Print

2022 Aug.
Chemrxiv

Aug 11, 2021.
bioRxiv

Identification of a Novel Susceptibility Marker for SARS-CoV-2 Infection in Human Subjects and Risk Mitigation with a Clinically Approved JAK Inhibitor in Human/Mouse Cells. [Abstract]

2020 Dec 9:2020.12.09.416586. PMID: 33330862
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 116.67 mg/mL (373.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 2.5 mg/mL (8.00 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2013 mL

16.0067 mL

32.0133 mL

5 mM

0.6403 mL

3.2013 mL

6.4027 mL

10 mM

0.3201 mL

1.6007 mL

3.2013 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 5 mg/mL (16.01 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Kinase activity is recorded via a competition binding assay of selected kinases that are fused to a proprietary tag. Measurements of the amount of kinase binds to an immobilized, active-site directed ligand in the presence and absence of the test compound (e.g., Tofacitinib) provide a % of DMSO control for binding of ligand. Activities between 0 and 10 are selected for Kd determinations. Dendrogram representations are generated by an in-house visualization tool designated PhyloChem^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Human CD4⁺ positive cells are enriched from peripheral blood mononuclear cells obtained from a healthy donor by magnetic separation (CD4⁺ MACS beads). CD4⁺ cells are activated for 3 days with plate bound anti-CD3 and anti CD28 antibodies (5 ug/mL each), and then expanded for another 4 days in the presence of IL-2 (50 U/mL). Cells are rested overnight in 1% RPMI, and pre-incubated with Tofacitinib or DMSO control for 1 hour at indicated concentrations (5 nM, 50 nM, 500 nM; DMSO concentration is equal in all preparations) and then activated with IL-2 (1000 u/mL) or IL-12 (100 ng/mL) for 15 minutes. Cells (10×10⁶/condition) are lysed in 1% Triton-x lysis buffer and equal amounts of cell lysate are run in NuPage Bis-Tris gel (4-12% gradient). Proteins are transferred onto nitrocellulose membrane. Detection is done with indicated antibodies using Odyssey western blotting system^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]^[3]

Mice^[2]
Female BALB/c mice (6-8 weeks old) are used. Mice receive Tofacitinib in PEG300 (100 mg/mL) or vehicle alone (PEG300) by osmotic pump infusion (Alzet Model 2004, 0.25 μL/hour, 28 days). Four days prior to immunization, mice are anesthetized and their dorsal surface is shaved. A one cm incision is made on the back to create a subcutaneous pocket and insert the pump. The incision site is closed with wound clips. Mice are injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, 50 μL of blood is drawn to obtain serum samples. Sera are stored at −80°C until analyzed.
Rats^[3]
Adjuvant-induced arthritis (AIA) is induced in female Lewis rats. Rats are randomized according to hind paw volume and assigned to Tofacitinib or vehicle treatment regimens. Groups of 7-8 rats per treatment group, and normal naive rats (n=4 per group), are euthanized either 4 hours, 4 days, or 7 days after beginning treatment (days 16, 20, and 23 after immunization, respectively). Tofacitinib is suspended in 0.5% methylcellulose/0.025% Tween 20 for in vivo studies. Once-daily oral administration of vehicle or Tofacitinib (6.2 mg/kg) is initiated on day 16 following immunization and continued through day 23. Paw volumes are reassessed 4 and 7 days after the beginning of treatment (days 20 and 23 after immunization, respectively). For micro-computed tomography (micro-CT) imaging, as well as tartrate-resistant acid phosphatase (TRAP) staining in paw tissue, AIA is induced in a separate cohort of Lewis rats.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jiang JK, et al. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem. 2008 Dec 25;51(24):8012-8. [Content Brief]

[2]. Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193(1):48-55. [Content Brief]

[3]. LaBranche TP, et al. JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production. Arthritis Rheum. 2012 Nov;64(11):3531-42. [Content Brief]

[4]. Calama E, et al. Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. Pulm Pharmacol Ther. 2017 Apr;43:60-67. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	3.2013 mL	16.0067 mL	32.0133 mL	80.0333 mL
Ethanol / DMSO	5 mM	0.6403 mL	3.2013 mL	6.4027 mL	16.0067 mL
DMSO	10 mM	0.3201 mL	1.6007 mL	3.2013 mL	8.0033 mL
	15 mM	0.2134 mL	1.0671 mL	2.1342 mL	5.3356 mL
	20 mM	0.1601 mL	0.8003 mL	1.6007 mL	4.0017 mL
	25 mM	0.1281 mL	0.6403 mL	1.2805 mL	3.2013 mL
	30 mM	0.1067 mL	0.5336 mL	1.0671 mL	2.6678 mL
	40 mM	0.0800 mL	0.4002 mL	0.8003 mL	2.0008 mL
	50 mM	0.0640 mL	0.3201 mL	0.6403 mL	1.6007 mL
	60 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3339 mL
	80 mM	0.0400 mL	0.2001 mL	0.4002 mL	1.0004 mL
	100 mM	0.0320 mL	0.1601 mL	0.3201 mL	0.8003 mL

Keywords

Tofacitinib

100 Cited Publications

100 mg Angebot einholen

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Tofacitinib

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Publications Citing Use of MedChemExpress (MCE) Tofacitinib

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (100)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tofacitinib Related Classifications

HY-40354 Related Classifications