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.
|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.|
|Incubation time||72 hours|
|Animal models||Mauritius-origin adult cynomolgus monkeys|
|Formulation||0.5% methylcellulose in distilled water|
|Dosages||10, 30 mg/kg/d|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO >50 mg/mL
Ethanol >50 mg/mL
The JAK kinase inhibitor CP-690,550 suppresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation.
Manshouri T, et al. Cancer Sci. 2008 Jun;99(6):1265-73. PMID: 18482053.
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WHI-P97 is a JAK3 inhibitor with an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays.
SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
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