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
Synonyme(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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5 MG
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About This Item
Formule empirique (notation de Hill) :
C16H20N6O · C6H8O7
Numéro CAS:
Poids moléculaire :
504.49
Numéro MDL:
Code UNSPSC :
12352200
ID de substance PubChem :
Nomenclature NACRES :
NA.77
144,00 $
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Nom du produit
Tofacitinib citrate, ≥98% (HPLC)
Niveau de qualité
Essai
≥98% (HPLC)
Forme
powder
Couleur
white to beige
Solubilité
DMSO: 5 mg/mL (clear solution; warmed)
Température de stockage
room temp
Chaîne 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
Clé InChI
SYIKUFDOYJFGBQ-YLAFAASESA-N
Informations sur le gène
human ... JAK1(3716) , JAK2(3717) , JAK3(3718) , TYK2(7297)
Description générale
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]
Actions biochimiques/physiologiques
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).
Caractéristiques et avantages
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.
Autres remarques
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.
Mention d'avertissement
Warning
Mentions de danger
Conseils de prudence
Classification des risques
Acute Tox. 4 Oral - Repr. 2
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 1
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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Les clients ont également consulté
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)
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
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)
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)
Articles
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
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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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