1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Tofacitinib citrate (Synonyms: Tasocitinib citrate; CP-690550 citrate)

Cat. No.: HY-40354A Purity: 99.92%
Handling Instructions

Tofacitinib citrate inhibits JAK3 with IC50 of 1 nM while inhibiting JAK2, JAK1, Rock-II and Lck with IC50 values of 20 nM, 112 nM, 3,400 nM and 3,870 nM, respectively.

For research use only. We do not sell to patients.

Tofacitinib citrate Chemical Structure

Tofacitinib citrate Chemical Structure

CAS No. : 540737-29-9

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Other Forms of Tofacitinib citrate:

    Tofacitinib citrate purchased from MCE. Usage Cited in: Pulm Pharmacol Ther. 2017 Apr;43:60-67.

    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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Tofacitinib citrate inhibits JAK3 with IC50 of 1 nM while inhibiting JAK2, JAK1, Rock-II and Lck with IC50 values of 20 nM, 112 nM, 3,400 nM and 3,870 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)

    In Vitro

    Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (Kd). The report includes additional binding for Tofacitinib at Camk1 (Kd of 5,000 nM), DCamkL3 (Kd of 4.5 nM), Mst2 (Kd of 4,300 nM), Pkn1 (Kd of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (Kd of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (Kd of 1,200 nM), Snark (Kd of 420 nM), Tnk1 (Kd of 640 nM) and Tyk2 (Kd of 620 nM)[1]. K562, KCL22, and THP-1 cells are exposed to different doses of Imatinib (IMA) or JAK inhibitors for 72 h to quantify the effects of tyrosine kinase inhibitor (TKI) activity. Cell growth inhibition is then evaluated using the MTT assay. The proliferation of K562 and KCL22 cells, but not THP-1 cells, is inhibited by IMA in a concentration-dependent manner. The IC50 value of IMA is 0.28 µM for K562 and 0.17 µM for KCL22. Although treatment with Tofacitinib (TOF) or Ruxolitinib (RUX) alone does not suppress cell proliferation, both Tofacitinib and Ruxolitinib make the K562 and KCL22 more sensitive to IMA[4].

    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].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    H2O : 5 mg/mL (9.91 mM; Need ultrasonic and warming)

    DMSO : ≥ 122.5 mg/mL (242.82 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9822 mL 9.9110 mL 19.8220 mL
    5 mM 0.3964 mL 1.9822 mL 3.9644 mL
    10 mM 0.1982 mL 0.9911 mL 1.9822 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    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].

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

    Cell Assay
    [4]

    Cell survival assay is performed using MTT. Briefly, K562, KCL22, and THP-1 cells (1×105 cells/well) are plated onto 96-well microplates and treated with or without IMA (0.06-1.0 μM) and/or Tofacitinib (10-1,000 nM) or RUX (10-1,000 nM) for 72 h at 37°C in a humidified 5% (v/v) CO2 atmosphere. The medium (200 µL) is then incubated with 10 µL of 5 mg/ml MTT solution for 4 h at 37°C. After being centrifuged at 352 g for 5 min, the culture medium is removed, and 100 µL of DMSO are added to each well to dissolve the formazan. Absorbance is measured at 570 nm using a microplate reader. The results are expressed as percentages[4].

    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 (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). 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.

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

    References
    Molecular Weight

    504.49

    Formula

    C₂₂H₂₈N₆O₈

    CAS No.

    540737-29-9

    SMILES

    O=C(CC#N)N1C[[email protected]](N(C2=C3C(NC=C3)=NC=N2)C)[[email protected]](C)CC1.O=C(CC(C(O)=O)(O)CC(O)=O)O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.92%

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    Product Name:
    Tofacitinib citrate
    Cat. No.:
    HY-40354A
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    Tofacitinib citrate

    Cat. No.: HY-40354A