Tofacitinib citrate inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. Tofacitinib citrate prevents mixed lymphocyte reaction with IC50 of 87 nM. Tofacitinib citrate inhibits interleukin-6-induced phosphorylation of STAT1 and STAT3 with IC50 of 23 nM and 77 nM, respectively. Tofacitinib citrate decrease a delayed-type hyper-sensitivity response and extended cardiac allograft survival in murine models. CP-690,550 induced a significant pro-apoptotic effect on murine FDCP-EpoR cells carrying JAK2(V617F), whereas a lesser effect was observed for cells carrying wild-type JAK2.
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Tofacitinib citrate purchased from AbMole
Cell Experiment | |
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Cell lines | FDCP-EpoR JAK2WT and JAK2V617F cell lines |
Preparation method | Using identical culture conditions for both FDCP-EpoR JAK2WT and JAK2V617F cell lines perform determination of growth inhibition by Tofacitinib citrate is performed. Briefly, culturing 1 × 105 cells/mL in 96-well flat-bottom plates at 37 °C in a humidified 5% CO2 atmosphere using RPMI 1640 supplemented with 1.25% FCS, and 5% WEHI supernatant. It's necessary to prevent binding between Tofacitinib citrate and serum proteins to decrease FCS concentration . Terminating growth inhibition assays by addition of 20 μL CellTiter96 One Solution Reagent. Incubating Flat-bottom plates for an additional 3 hours for MTT assay. Determining absorbance at 595 nm on a BioTek Synergy-HT microplate reader. Results are the average standard deviation of three independent determinations. |
Concentrations | 0-4 μM |
Incubation time | 72 hours |
Animal Experiment | |
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Animal models | Mauritius-origin adult cynomolgus monkeys |
Formulation | 0.5% methylcellulose in distilled water |
Dosages | 10, 30 mg/kg/d |
Administration | Oral gavage |
Molecular Weight | 504.49 |
Formula | C22H28N6O8 |
CAS Number | 540737-29-9 |
Solubility (25°C) | DMSO >30 mg/mL Water 2 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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