Tofacitinib (CP-690550,Tasocitinib)

Licensed by Pfizer Catalog No.S2789

Tofacitinib (CP-690550,Tasocitinib) Chemical Structure

Molecular Weight(MW): 312.37

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

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In DMSO USD 91 In stock
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Cited by 59 Publications

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Biological Activity

Description Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.
Targets
JAK3 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 JAK1 [1]
(Cell-free assay)
1 nM 20 nM 112 nM
In vitro

CP-690550 is a specific, orally inhibitor of JAK3, it is 20- to 100-fold less potent for JAK2 and JAK1 with IC50 of 20 nM and 112 nM, respectively. CP-690550 doesn't have potent activity against 30 other kinases (all median IC50 > 3000 nM). CP-690,550 inhibits IL-2–induced proliferation with 30-fold greater potency than its effects on GM-CSF–induced proliferation. [1] CP-690550 effectively inhibits a murine mixed lymphocyte reaction (MLR) (IC50 = 91 nM). [2] CP-690550 potently inhibits IL-4 induced upregulation of CD23 (IC50=57 nM) and class II major histocompatibility complex (MHCII) expression (IC50=71 nM) on murine B cells. [3] A recent research indicates low dose of CP-690550 accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation. [4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CD4+ T  NHrSZppHfW6ldHnvckBCe3OjeR?= M3u3flIxNzFyMD:1NFAhdk1? NF;OWnA1QCCq M1XLV4lvcGmkaYTzJJRp\SCuZY\lcJMhd2ZiIFnMMVQtKEmITj5Ot{whUUxvMUfBJIFv\CCLTD2yNi=> NHnJb44zOTh6NEW4NC=>
CD4+ T  NF3TOlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmxNFAwPTByIH7N NIfsPYE1QCCq MXPpcohq[mm2czDhcpRqNUOGMz3pcoR2[2WmIFPEOEvDqFRiY3XscEBxem:uaX\ldoF1cW:w MoDpNlE5QDR3OEC=
CD4+ T  MWjGeY5kfGmxbjDBd5NigQ>? MlX6NVAxKG6P NWH4d5dTOjRxNEigbC=> NEPVVlRi[nKxZ3H0[ZMhS0R|LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIGPURXR{ NECxWngzOTh6NEW4NC=>
T cells MYnGeY5kfGmxbjDBd5NigQ>? MVWwMlEwOC5|L{Gg{txO MYCyOEBp NHHYNVdlcXO{dYD0d{DPu2NvY3jhbY4h[3m2b3vpcoUhe2mpbnHsbY5o MYOyNVM5OzJ2MR?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
JAK3 / STAT5 / p-STAT5 ; 

PubMed: 27732937     


The following cell lines: EBV-negative B cell line (BJAB), EBV-transformed lymphoblastoid cell line (LCL), EBV-negative T cell lines (Jurkat and MOLT4), EBV-positive T cell lines (SNT15 and SNT16), EBV-negative NK cell line (KHYG1), and EBV-positive NK cell lines (KAI3 and SNK6), were treated without (−) or with (+) 1 μM tofacitinib for 24 h and cell lysates were then immunoblotted for the indicated proteins.

LMP1 / EBNA1 / BZLF1 ; 

PubMed: 27732937     


SNT13, SNT15, SNT16, KAI3 and SNK6 cell lines were treated with 5 μM tofacitinib for 48 h, and cell lysates were immunoblotted for LMP1, EBNA1 and BZLF1. Actin was blotted as a loading control.

JAK3 / p-JAK3 / STAT3 ; 

PubMed: 26082451     


CTCL cell lines were subjected to western blot (tofacitinib 10, 100, 200 nM) (G) after 48 hours of treatment.

27732937 26082451
Growth inhibition assay
Cell number ; 

PubMed: 27732937     


BJAB, LCL, Jurkat, SNT15, KHYG1 and KAI3 cells were treated with the indicated concentrations of tofacitinib, and viable cells were counted at the indicated times using the trypan blue exclusion test. Values are means ± SE of the results from triplicate experiments. *P < 0.05 as compared with DMSO-treated cells.

27732937
In vivo In a murine model of heterotopic heart transplantation (DBA2 donor heart into C57/BL6 host), CP-690550 results in a dose-dependent increase in survival of transplanted hearts.The EC50 (drug concentration in blood at which 50% of mice will maintain their graft for >28 days) to be ~60 ng/mL.CP-690550 prevents rejection of allogeneic kidneys in nonhuman primate (NHPs, macaca fascicularis) (MST of 62 and 83 days for the 50 to 100 ng/ml groups and 200 to 400 ng/ml groups, respectively). [1] Mice chronically dosed with CP-690550 (1.5-15 mg/kg/day) demonstrates dose and time-dependent alterations in lymphocyte subsets when examined by flow cytometry. The most dramatic change observed is a 96% reduction in splenic NK1.1+TCRb-cell numbers following 21 days of treatment. Delayed-type hypersensitivity (DTH) responses in sensitized mice are reduced in a dose-dependent manner following treatment with CP-690550 (1.87–30 mg/kg, s.c.). Extended survival of neonatal Balb/c hearts implanted into the ear pinna of MHC mismatched C3H/HEN mice is observed with CP-690550 monotherapy (10–30 mg/kg/day), but improved upon combination with cyclosporin (10 mg/kg/day). [2]

Protocol

Kinase Assay:

[1]
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JAK3 Kinase Assay:

A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays.
Cell Research:

[1]
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  • Cell lines: Human T blasts cell
  • Concentrations: 0-4000 nM
  • Incubation Time: 4 days
  • Method:

    To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 106/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO2 incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO2 incubator, after which 50 mL of 3H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period.


    (Only for Reference)
Animal Research:

[1]
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  • Animal Models: DBA/2 and C57/BL6 mice
  • Formulation: CP-690550 is dissolved in polyethylene glycol 300.
  • Dosages: 0-136 ng/mL
  • Administration: Administered via osmotic minipump infusion
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL warmed (198.48 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 312.37
Formula

C16H20N6O
CAS No. 477600-75-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04111614 Not yet recruiting Drug: Tofacitinib tablet|Drug: Tofacitinib Oral Solution Healthy Pfizer October 9 2019 Phase 1
NCT03681275 Recruiting Drug: Tofacitinib 5 mg|Drug: Placebo to match Tofacitinib Diaphragm Injury Stanford University September 3 2019 Phase 1
NCT04047121 Active not recruiting -- Rheumatoid Arthritis Pfizer May 20 2019 --

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Frequently Asked Questions

  • Question 1:

    I was just wondering what the main differences between S2789 and S5001?

  • Answer:

    S2789(Tofacitinib (CP-690550)) is the base form of S5001 (Tofacitinib (CP-690550) Citrate). The biological activity of these two compounds are same. The S5001 (Tofacitinib (CP-690550) Citrate) is more suitable for oral administration.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID