Tofacitinib (CP-690550) Citrate 化学構造
分子量: 504.49




Quality Control & MSDS


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製品説明 Tofacitinib (CP-690550) Citrate は、1nMのIC50によるJAK3の強力なJAKキナーゼ阻害剤です。
ターゲット JAK3
IC50 1 nM [1]
In vitro試験 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 treatment of murine factor-dependent cell Patersen–erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 leads to prevention of cell proliferation with IC50 of 2.1 µM and 0.25 µM, respectively. Tofacitinib citrate inhibits interleukin-6-induced phosphorylation of STAT1 and STAT3 with IC50 of 23 nM and 77 nM, respectively. Moreover, Tofacitinib citrate generates a significant pro-apoptotic effect on murine FDCP-EpoR cells carrying JAK2VV617F, whereas a lesser effect is observed for cells carrying wild-type JAK2. This activity is coupled with the inhibition of phosphorylation of the key JAK2V617F-dependent downstream signaling effectors signal transducer and activator of transcription (STAT)3, STAT5, and v-akt murine thymoma viral oncogene homolog (AKT). [2] Additionally, Tofacitinib citrate prevents IL-15-induced CD69 expression in human and cynomolgus monkey NK and CD8+ T cells in vitro. [3]
In vivo試験 Tofacitinib citrate decrease a delayed-type hyper-sensitivity response and extended cardiac allograft survival in murine models. Furthermore, Tofacitinib citrate treatment of ex-vivo-expanded erythroid progenitors from JAK2V617F-positive PV patients results in specific, antiproliferative (IC50 = 0.2 μM) and pro-apoptotic activity. In contrast, expanded progenitors from healthy controls are less sensitive to Tofacitinib citrate in proliferation (IC50 > 1.0 μM), and apoptosis assays.[2] During 2 weeks of Tofacitinib citrate dosing at 10 and 30 mg/kg/d, a significant, time-dependent decrease in NK cell numbers relative to vehicle treatment is observed. Effector memory CD8+ cell numbers in the Tofacitinib citrate-treated group are 55% less than those observed in animals treated with vehicle.[3]
臨床試験 Tofacitinib citrate is under a Phase II clinical trial in the treatment of chronic plaque psoriasis.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Enzyme assays The JAK1, JAK2, and JAK3 kinase assays utilize a protein expressed in baculovirus-infected SF9 cells (a fusion protein of GST and the catalytic domain of human JAK enzyme) purified by affinity chromatography on glutathione−Sepharose. The substrate for the reaction is polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates are washed three times, and JAK enzyme is added to the wells, which contained 100 μL of kinase buffer (50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM sodium orthovanadate). For Tofacitinib citrate, it is also added for kinase assay at different doses. After incubation at room temperature for 30 min, the plates are washed three times. The level of phosphorylated tyrosine in a given well is determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody.

細胞アッセイ: [2]

細胞株 FDCP-EpoR JAK2WT and JAK2V617F cell lines
濃度 0-4 μM
反応時間 72 hours
実験の流れ Determination of growth inhibition by Tofacitinib citrate is performed using identical culture conditions for both FDCP-EpoR JAK2WT and JAK2V617F cell lines. Briefly, 1 × 105 cells/mL are cultured 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. Decreased FCS concentration is necessary to prevent binding between Tofacitinib citrate and serum proteins. Growth inhibition assays are terminated by addition of 20 μL CellTiter96 One Solution Reagent. Flat-bottom plates are incubated for an additional 3 hours for MTT assay. Absorbance is determined at 595 nm on a BioTek Synergy-HT microplate reader. Results are the average standard deviation of three independent determinations.

動物実験: [2]

動物モデル Mauritius-origin adult cynomolgus monkeys
製剤 0.5% methylcellulose in distilled water
投薬量 10, 30 mg/kg/d
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Tofacitinib (CP-690550) Citrate SDF
分子量 504.49


CAS No. 540737-29-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL warming (198.21 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile citrate

カスタマーフィードバック (4)

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Source Biochem Biophy Res Commun, 2010, 402, 500–506. Tofacitinib (CP-690550) Citrate purchased from Selleck
Method RT-PCR, ELISA, TTC staining, Neurological assessment
Cell Lines γδT cells and activated memory T cells
Concentrations 10 μM
Incubation Time
Results CP-690550 efficiently suppressed IL-17 production by γδT cells as well as memory CD4+T cells.We investigated the effect of CP-690550 in ischemic brain damage in mice. CP-690550 or vehicle was injected intra-peritoneally after I/R. The degree of CBF reduction was similar in the two groups (Fig. B). As shown in Fig. 1C, the functional neurological deficit induced by I/R surgery was significantly improved in mice receiving CP-690550 7 days after MCAO compared to control mice. Infarct size was smaller in mice treated with CP-690550 3 days after MCAO than in untreated mice, as shown in Fig. D

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Source Dr. Akihiko Yoshimura of Akihiko Yoshimura. Tofacitinib (CP-690550) Citrate purchased from Selleck
Method Immunoblotting, real-time PCR
Cell Lines MC3T3-E1 cells
Concentrations 0-1000 nM
Incubation Time 24 h
Results The STAT3 inhibitor CP690,550 inhibits arthritis in vivo and the expression of IL-6 cytokine family in vitro.

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Source Saraswati Sukumar of Johns Hopkins University School of Medicine. Tofacitinib (CP-690550) Citrate purchased from Selleck
Method real-time PCR, ELISA, Western blot
Cell Lines hind paws cells of mice
Concentrations 15mg/kg/day
Incubation Time 2 weeks
Results STAT3-inhibition antagonizes arthritis effects in vivo.

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Source Dr. Akihiko Yoshimura of Akihiko Yoshimura. Tofacitinib (CP-690550) Citrate purchased from Selleck
Method Histopathology, fluorescent immunohistochemistry
Cell Lines DBA/J1 male mice
Concentrations 15mg/kg/day
Incubation Time 2 weeks
Results Joint destruction seen in the CIA model was rescued by CP690,550 treatment

文献中の引用 (34)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID