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Tofacitinib citrate

Cat. No. M3616
Tofacitinib citrate  Structure
Synonym:

CP-690550 citrate

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 60 In stock
50mg USD 180 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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
Animal models Mauritius-origin adult cynomolgus monkeys
Formulation 0.5% methylcellulose in distilled water
Dosages 10, 30 mg/kg/d
Administration Oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 504.49
Formula C22H28N6O8
CAS Number 540737-29-9
Purity >98%
Solubility DMSO >50 mg/mL
Ethanol >50 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tofacitinib citrate , CP-690550 citrate supplier, JAK, inhibitors

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