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

Name: Tofacitinib citrate
Brand: MedChemExpress
SKU: HY-40354A
Rating: 5.0 (49 reviews)

Cat. No.: HY-40354A Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 540737-29-9

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10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
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Based on 49 publication(s) in Google Scholar

Other Forms of Tofacitinib citrate:

48 Publications Citing Use of MCE Tofacitinib citrate

: Tofacitinib citrate 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.

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View All JAK Isoform Specific Products:

View All Isoforms

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 (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].
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].

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

Molecular Weight

504.49

Formula

C₂₂H₂₈N₆O₈

CAS No.

540737-29-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(CC#N)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C)[C@H](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, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 28.57 mg/mL (56.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

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

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: 50% PEG300 50% Saline
Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (287 KB) SDS (252 KB)

COA (256 KB) RP-HPLC (170 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[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]. Yagi K, et al. Pharmacological inhibition of JAK3 enhances the antitumor activity of STI571 in human chronic myeloid leukemia. Eur J Pharmacol. 2018 Apr 15;825:28-33. [Content Brief]

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	[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]. Yagi K, et al. Pharmacological inhibition of JAK3 enhances the antitumor activity of STI571 in human chronic myeloid leukemia. Eur J Pharmacol. 2018 Apr 15;825:28-33. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.9822 mL	9.9110 mL	19.8220 mL	49.5550 mL
H₂O / DMSO	5 mM	0.3964 mL	1.9822 mL	3.9644 mL	9.9110 mL
DMSO	10 mM	0.1982 mL	0.9911 mL	1.9822 mL	4.9555 mL
	15 mM	0.1321 mL	0.6607 mL	1.3215 mL	3.3037 mL
	20 mM	0.0991 mL	0.4955 mL	0.9911 mL	2.4777 mL
	25 mM	0.0793 mL	0.3964 mL	0.7929 mL	1.9822 mL
	30 mM	0.0661 mL	0.3304 mL	0.6607 mL	1.6518 mL
	40 mM	0.0496 mL	0.2478 mL	0.4955 mL	1.2389 mL
	50 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9911 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Tofacitinib citrate Related Classifications

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.

Keywords:

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

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

Customer Review

Other Forms of Tofacitinib citrate:

Tofacitinib citrate Related Antibodies

48 Publications Citing Use of MCE Tofacitinib citrate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Tofacitinib citrate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tofacitinib citrate Related Classifications

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