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PZ0017

Sigma-Aldrich

Tofacitinib citrate

≥98% (HPLC), powder, JAK3 inhibitor

Sinonimo/i:

(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

Formula empirica (notazione di Hill):
C16H20N6O · C6H8O7
Numero CAS:
Peso molecolare:
504.49
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77
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Nome del prodotto

Tofacitinib citrate, ≥98% (HPLC)

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

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

Temperatura di conservazione

room temp

Stringa SMILE

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
SYIKUFDOYJFGBQ-YLAFAASESA-N

Informazioni sul gene

Descrizione generale

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

Applicazioni

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]

Azioni biochim/fisiol

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).

Caratteristiche e vantaggi

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.

Altre note

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.

Pittogrammi

Health hazardExclamation mark

Avvertenze

Warning

Indicazioni di pericolo

Classi di pericolo

Acute Tox. 4 Oral - Repr. 2

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 1

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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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
Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo
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The mechanism of action of tofacitinib-an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis
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Articoli

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Domande

1–3 di 3 domande  
  1. After dissolving in DMSO. Does it need to filter it?

    1 risposta
    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.

      Utile?

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

    1 risposta
    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.

      Utile?

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

    1 risposta
    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.

      Utile?

Recensioni

Nessuna valutazione

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