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
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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Prodotti consigliati
Nome del prodotto
Tofacitinib citrate, ≥98% (HPLC)
Livello qualitativo
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
human ... JAK1(3716) , JAK2(3717) , JAK3(3718) , TYK2(7297)
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.
Avvertenze
Warning
Indicazioni di pericolo
Consigli di prudenza
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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I clienti hanno visto anche
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
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)
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
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)
Articoli
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
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After dissolving in DMSO. Does it need to filter it?
1 risposta-
Utile?
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What is the solution stability information for Product PZ0017?
1 risposta-
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?
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Can Tofacitinib citrate (dissolved in DMSO) also be kept on room temperature?
1 risposta-
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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