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Tofacitinib

Catalog No. T6321   CAS 477600-75-2
Synonyms: Janus kinase, JAK, Apoptosis, Tofacitinib, CP690550, Inhibitor, CP 690550, Tasocitinib, inhibit, CP-690550

Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.

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Tofacitinib, CAS 477600-75-2
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Purity: 98%
Biological Description
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Storage & Solubility Information
Description Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
Targets&IC50 JAK2:20 nM, JAK1:112 nM, JAK3:1 nM
Kinase Assay JAK3 Kinase Assay: A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays.
Cell Research To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 106/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10 mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO2 incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO2 incubator, after which 50 mL of 3H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period. (Only for Reference)
Synonyms Janus kinase, JAK, Apoptosis, Tofacitinib, CP690550, Inhibitor, CP 690550, Tasocitinib, inhibit, CP-690550
Molecular Weight 312.37
Formula C16H20N6O
CAS No. 477600-75-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 58 mg/mL (185.7 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Si H, Wang J, He R, et al. Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in oncology. 2021, 11: 807200-807200. 1. Changelian PS, et al, Science, 2003, 302(5646), 875-878. 2. Kdlacz E, et al, Am J Transplant, 2004, 4(1), 51-57. 2. Luschnig P, Kienzl M, Roula D, et al. The JAK1/2 inhibitor baricitinib suppresses eosinophil effector function and restricts allergen-induced airway eosinophilia. Biochemical Pharmacology. 2021: 114690. 3. Kudlacz E, et al, Eur J harmacol, 2008, 582(1-2), 154-161. 4. Yoshida H, et al, Biochem Biophys Res Commun, 2012, 418(2), 234-240. 5. Borie DC, et al, Transplantation, 2005, 80(12), 1756-1764. 6. Calama E, et al. Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. Pulm Pharmacol Ther. 2017 Apr;43:60-67.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library HIF-1 Signaling Pathway Compound Library TGF-beta/Smad Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library Neural Regeneration Compound Library Immunology/Inflammation Compound Library Anti-Metabolism Disease Compound Library Cell Cycle Compound Library

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