This is not a sterile product. Stock solutions should be filtered using a 0.22 um PTFE filter membrane for applications that require sterile reagents.
PZ0017
Tofacitinib citrate
≥98% (HPLC), powder, JAK3 inhibitor
Synonym(s):
(3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate salt, 3-[(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile citrate salt, CP-690550-10, Tasocitinib citrate salt
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About This Item
Empirical Formula (Hill Notation):
C16H20N6O · C6H8O7
CAS Number:
Molecular Weight:
504.49
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
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Product Name
Tofacitinib citrate, ≥98% (HPLC)
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL (clear solution; warmed)
storage temp.
room temp
SMILES string
OC(=O)CC(O)(CC(O)=O)C(O)=O.C[C@@H]1CCN(C[C@@H]1N(C)c2ncnc3[nH]ccc23)C(=O)CC#N
InChI
1S/C16H20N6O.C6H8O7/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16;7-3(8)1-6(13,5(11)12)2-4(9)10/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t11-,13+;/m1./s1
InChI key
SYIKUFDOYJFGBQ-YLAFAASESA-N
Gene Information
human ... JAK1(3716), JAK2(3717), JAK3(3718), TYK2(7297)
Related Categories
1 of 4
This Item | PZ0316 | PZ0195 | PZ0385 |
|---|---|---|---|
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| form powder | form powder | form powder | form powder |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level - |
| storage temp. room temp | storage temp. room temp | storage temp. room temp | storage temp. room temp |
| solubility DMSO: 5 mg/mL (clear solution; warmed) | solubility H2O: 5 mg/mL, clear (warmed) | solubility DMSO: >10 mg/mL (warmed) | solubility DMSO: 2 mg/mL, clear |
| color white to beige | color white to beige | color white to beige | color white to beige |
General description
Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.[1]
Application
Tofacitinib citrate has been used:
- as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studies[2]
- as a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan loss[3]
- as a Janus kinase inhibitor in MCF7 breast cancer cells[4]
Biochem/physiol Actions
Tofacitinib is a potent inhibitor of Janus kinase 3 (JAK3) with some JAK-1 inhibitory activity as well. It blocks downstream STAT signaling resulting in potent inhibition of inflammatory cytokines with resultant immunosuppressive and anti-inflammatory activity. Tofacitinib is being investigated for for several autoimmune disorders including, rheumatoid arthritis, psoriasis and dry eye.
Tofacitinib is a potent inhibitor of Janus kinase 3 (JAK3).
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Other Notes
Tofacitinib has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the Tofacitinib probe summary on the Chemical Probes Portal website.
Signal Word
Warning
Hazard Statements
Precautionary Statements
Hazard Classifications
Acute Tox. 4 Oral - Repr. 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Ji Sang Lee et al.
Pharmaceutics, 11(7) (2019-07-10)
This study investigated the pharmacokinetics of tofacitinib in rats and the effects of first-pass metabolism on tofacitinib pharmacokinetics. Intravenous administration of 5, 10, 20, and 50 mg/kg tofacitinib showed that the dose-normalized area under the plasma concentration-time curve from time
Phosphoproteome profiling reveals critical role of JAK-STAT signaling in maintaining chemoresistance in breast cancer
Nascimento AS, et al.
Testing, 8(70), 114756-114756 (2017)
Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo
Kjelgaard-Petersen CF, et al.
Biochemical Pharmacology (2018)
The mechanism of action of tofacitinib-an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis
Hodge JA, et al.
Clinical and Experimental Rheumatology, 34(2), 318-328 (2016)
Ben X Wang et al.
Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research, 37(4), 147-152 (2017-04-08)
Aicardi-Goutières syndrome (AGS) is an early-onset, genetic disease characterized by recurrent fever, multifocal lesions of the brain, and systemic autoimmunity. We report on 3 AGS patients, 2 siblings with an RNASEH2A gene mutation and 1 patient with a SAMHD1 gene
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After dissolving in DMSO. Does it need to filter it?
1 answer-
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What is the solution stability information for Product PZ0017?
1 answer-
Solution stability for this product in DMSO has not been tested in house. However, another supplier has conducted testing and recommends storing the stock solution below -20℃ for several months.
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Can Tofacitinib citrate (dissolved in DMSO) also be kept on room temperature?
1 answer-
Unfortunately, this product has not been internally tested for solution stability in DMSO. However, other sources recommend that stock solution can be stored below -20°C for several months.
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