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PZ0017

Sigma-Aldrich

Tofacitinib citrate

≥98% (HPLC), powder, JAK3 inhibitor

Sinônimo(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

Fórmula empírica (Notação de Hill):
C16H20N6O · C6H8O7
Número CAS:
Peso molecular:
504.49
Número MDL:
Código UNSPSC:
12352200
ID de substância PubChem:
NACRES:
NA.77
Preço e disponibilidade não estão disponíveis no momento.

Nome do produto

Tofacitinib citrate, ≥98% (HPLC)

Ensaio

≥98% (HPLC)

Formulário

powder

cor

white to beige

solubilidade

DMSO: 5 mg/mL (clear solution; warmed)

temperatura de armazenamento

room temp

cadeia de caracteres SMILES

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

chave InChI

SYIKUFDOYJFGBQ-YLAFAASESA-N

Informações sobre genes

Descrição geral

Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.[1]

Aplicação

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]

Ações bioquímicas/fisiológicas

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).

Características e benefícios

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.

Outras notas

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.

Pictogramas

Health hazardExclamation mark

Palavra indicadora

Warning

Frases de perigo

Classificações de perigo

Acute Tox. 4 Oral - Repr. 2

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 1

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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Visite a Biblioteca de Documentos

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)
Usir S Younis et al.
AAPS PharmSciTech, 20(5), 167-167 (2019-04-18)
Preformulation studies on tofacitinib citrate, a small molecule JAK3 specific inhibitor, have not been previously reported in literature. We therefore conducted several preformulation studies on tofacitinib citrate, and its free base, to better understand factors that affect its solubility, stability
Binding of Janus kinase inhibitor tofacitinib with human serum albumin: multi-technique approach
Abdelhameed AS, et al.
Journal of Biomolecular Structure & Dynamics, 34(9), 2037-2044 (2016)

Artigos

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Questions

1–3 of 3 Questions  
  1. After dissolving in DMSO. Does it need to filter it?

    1 answer
    1. 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.

      Helpful?

  2. What is the solution stability information for Product PZ0017?

    1 answer
    1. 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.

      Helpful?

  3. Can Tofacitinib citrate (dissolved in DMSO) also be kept on room temperature?

    1 answer
    1. 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.

      Helpful?

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