Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
無料サンプル 1 mg | |||||
5 mg | 在庫あり | ¥ 7,000 | |||
10 mg | 在庫あり | ¥ 11,000 | |||
25 mg | 在庫あり | ¥ 13,500 | |||
50 mg | 在庫あり | ¥ 18,000 | |||
100 mg | 在庫あり | ¥ 22,500 | |||
200 mg | 在庫あり | ¥ 34,000 | |||
500 mg | 在庫あり | ¥ 63,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,000 |
説明 | Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis. |
ターゲット&IC50 | JAK2:20 nM, JAK1:112 nM, JAK3:1 nM |
キナーゼ試験 | 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. |
細胞研究 | 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) |
別名 | Tasocitinib, CP-690550 |
分子量 | 312.37 |
分子式 | C16H20N6O |
CAS No. | 477600-75-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 58 mg/mL (185.7 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
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Tofacitinib 477600-75-2 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Src ROCK CP 690550 Janus kinase Inhibitor inhibit Tasocitinib CP690550 CP-690550 inhibitor