2. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Apoptosis
    Anti-infection
  3. JAK
    Apoptosis
    Bacterial
    Fungal
    Influenza Virus
  4. Tofacitinib citrate

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

Cat. No.: HY-40354A Purity: 99.98%
COA Handling Instructions

Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

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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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
10 mg USD 66 In-stock
50 mg USD 106 In-stock
100 mg USD 145 In-stock
200 mg USD 198 In-stock
500 mg USD 370 In-stock
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Customer Review

Based on 42 publication(s) in Google Scholar

Other Forms of Tofacitinib citrate:

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Tofacitinib citrate

IP

    Tofacitinib citrate purchased from MCE. 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.

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

    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 STI571 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 INCB018424 alone does not suppress cell proliferation, both Tofacitinib and INCB018424 make the K562 and KCL22 more sensitive to IMA[4].

    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].

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

    504.49

    Appearance

    Solid

    Formula

    C22H28N6O8
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
    Solvent & Solubility
    In Vitro: 

    DMSO : 28.57 mg/mL (56.63 mM; Need ultrasonic)

    H2O : 3.33 mg/mL (6.60 mM; Need ultrasonic)

    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.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

    • 4.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

    • 5.

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

      Solubility: ≥ 1.43 mg/mL (2.83 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.98%

    COA (256 KB) RP-HPLC (170 KB)

    Handling Instructions (2659 KB)
    References
    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
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Tofacitinib540737-29-9TasocitinibCP-690550CP690550CP 690550JAKApoptosisBacterialFungalInfluenza VirusJanus kinaseInhibitorinhibitorinhibit

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