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Tofacitinib

Catalog No. T6321 CAS 477600-75-2

Synonyms: CP-690550, Tasocitinib

Purity 100.00% Datasheet MSDS

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

Tofacitinib, CAS 477600-75-2

Pack Size	Availability	Price/USD
5 mg	In stock	50.00
10 mg	In stock	60.00
25 mg	In stock	75.00
50 mg	In stock	90.00
100 mg	In stock	130.00
200 mg	In stock	180.00
500 mg	In stock	306.00
1 mL * 10 mM (in DMSO)	In stock	69.00

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Purity 100.00%

HNMR HPLC COA Datasheet MSDS

Purity 99.00%

HNMR LCMS COA Datasheet MSDS

Biological Description

Chemical Properties

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Description	Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
Targets&IC50	JAK1 :ic50 112nM, JAK2 :ic50 20nM, JAK3 :ic50 1nM, Lck :ic50 3.87μM, ROCK2 :ic50 3.4μM,
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 10mg/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) Cell lines: Human T blasts cell
Animal Research	Animal Model: DBA/2 and C57/BL6 mice

Synonyms	CP-690550, Tasocitinib
Purity	99.00%
Appearance	solid
Molecular Weight	312.37
Formula	C16H20N6O
CAS No.	477600-75-2

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 58 mg/mL (185.7 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

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

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature

1. Changelian PS, et al, Science, 2003, 302(5646), 875-878. 2. Kdlacz E, et al, Am J Transplant, 2004, 4(1), 51-57. 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. Kudlacz E, et al. Am J Transplant, 2004, 4(1), 51-57. 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：

Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Endocrinology-Hormones Library Epigenetics Compound Library FDA-approved Drug Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Angiogenesis related Compound Library JAK STAT Compound Library Cell cycle related Compound Library

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(R)-Ruxolitinib Momelotinib Filgotinib WHI-P154 Fedratinib Oclacitinib WHI-P258 WHI-P131

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