Tofacitinib (CP-690550) Citrate

Licensed by Pfizer Catalog No.S5001

Tofacitinib (CP-690550) Citrate Chemical Structure

Molecular Weight(MW): 504.49

Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.

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In DMSO USD 191 In stock
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Cited by 34 Publications

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  • CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.

     

     

    Biochem Biophy Res Commun 2010 402, 500–506. Tofacitinib (CP-690550) Citrate purchased from Selleck.

    The STAT3 inhibitor CP690,550 inhibits arthritis in vivo and the expression of IL-6 cytokine family in vitro. (A) Whole-cell lysates from MC3T3-E1 cells stimulated with IL-1β (10 ng/ml) plus CP690,550 at the indicated concentrations were analyzed by immunoblotting to detect pSTAT3 and STAT3. Actin served as an internal control. (B) 6-week-old DBA/1 male mice were given an initial injection of type 2 collagen on day -21, and arthritis was induced with a second injection on day 0. Vehicle or CP690,550 (15 mg/kg/day) was administered intraperitoneally once daily for 2 weeks from day 0 (n = 4 per group). Arthritis scores were measured three times a week. (C and D) Total RNA was prepared from primary osteoblasts treated with IL-1β (10ng/ml), TNFα (10 ng/ml) or OSM (50 ng/ml) with (+) or without (-) CP690,550 (100nM) for 24 hours, and IL-6 expression relative to β-actin was analyzed by quantitative real-time PCR. Data are means ±SD of IL-6/β-actin. (*P < 0.001; n = 3). (E) IL-6 protein levels in the supernatant of osteoblasts treated with IL-1β (left panel) or TNF (right panel) plus indicated concentrations of CP690,550 for 24 hours were assessed by ELISA. Data are means ±SD of IL-6 (pg/ml).

    Dr. Akihiko Yoshimura of Akihiko Yoshimura. Tofacitinib (CP-690550) Citrate purchased from Selleck.

  • STAT3-inhibition antagonizes arthritis effects in vivo. (A) 6-week-old DBA/J1 male mice were given initial injection of type 2 collagen on day -21, and arthritis was induced with a second injection on day 0. Vehicle or CP690,550 (15mg/kg/day) was administered intraperitoneally once daily for 2 weeks from day 7 (n = 4per group). Arthritis scores were measured three times a week. (B) Total RNA was prepared from the tissue of hind paws of CIA induced mice after 2 weeks of treatment by vehicle or CP690,550, and expression of IL-6 cytokine families (IL-6, OSM, IL-11 and LIF) relative to β-actin was analyzed by a quantitative real-time PCR. (C) IL 6 serum levels in sera of CIA induced mice after 2 weeks of treatment by vehicle or CP690,550 were assessed by ELISA. (D) Specimens of ankle joints from CIA mice treated with vehicle or CP690,550 for 2 weeks were subjected to immunofluorescence staining for pSTAT3. Nuclei were visualized by TOTO3. Bar, 100 μm. (E) Whole cell lysates were made from ankle joint tissues of CIA mice treated with or without CP690,550 for 2 weeks. Phosphorylated-STAT3 was then analyzed by western blot (upper panel) and ELISA (lower panel). Results are representative of at least three independent experiments.

    Saraswati Sukumar of Johns Hopkins University School of Medicine. Tofacitinib (CP-690550) Citrate purchased from Selleck.

    CP690,550 is effective in treating collagen-induced arthritis in vivo. 6-week-old DBA/J1 male mice were given an initial injection of type 2 collagen on day 21 and arthritis was induced with a second injection on day 0. Vehicle or CP690,550 (15mg/kg/day) was administered interperitoneally once daily for 2 weeks from day 0 (n = 4 per group). Tissue specimens from the ankle of CIA mice administered vehicle or CP690,550 were stained with safranin O and methyl green. Bar, 100 μM. Representatives of at least two independent experiments are shown.

    Dr. Akihiko Yoshimura of Akihiko Yoshimura. Tofacitinib (CP-690550) Citrate purchased from Selleck.

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description Tofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively.
Targets
JAK3 [1]
(Cell-free assay)
JAK2 [4]
(Cell-free assay)
1 nM 20 nM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells MW\GeY5kfGmxbjDhd5NigQ>? NUjRbndiOzBibXnudy=> MofGTY5pcWKrdHnvckBw\iCqdX3hckBIW1RvZoXz[YQhUkGNMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkmgZ4VtdHNidYPpcocheG:ueXfseZRidWmlIHHjbYQufHm{b4PpcoUh[XNic4Xid5Rz[XSnIHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEurPUCuOEBvVS5? M3rCUlI{PjZ6NEi0
Sf9 cells NEX4VWxHfW6ldHnvckBie3OjeR?= NVvnXoxCQTBibXnudy=> NUfoPVhRUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJGdUXC22YXfn[YQhUkGNMzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGJqd3Srbj3MR{1GWUWGRWDFS2R[TkWZTFWgZZMhe3Wkc4TyZZRmKGGodHXyJFkxKG2rboOgZpkhXFJvRmLFWEBie3OjeTygTWM2OD1yLk[gcm0v M3nGd|IzODh5N{Ww
SF21 cells MYTGeY5kfGmxbjDhd5NigQ>? M3zMRlExKG2rboO= MYPJcohq[mm2aX;uJI9nKEqDS{KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hW0Z{MTDj[YxteyC3c3nu[{BDcW:2aX6tT2FKTVSGS1XZXXRXU0RiYYOgd5Vje3S{YYTlJIFv\CCdM{PQ[4FudWGfQWTQJIlv[3WkYYTl[EBnd3JiMUCgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCWb4Djc5VvfCCjbnHsfZNqeyxiSVO1NF01KG6PLh?= NIrYeHQzOzV2MU[3NC=>
human MO7 cells MlPXSpVv[3Srb36gZZN{[Xl? M1zaRWlvcGmkaYTpc44hd2ZiSnHrN{1u\WSrYYTl[EBKVDF3LXnu[JVk\WRiU4TheFUheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1QPyClZXzsd{BjgSClZXzsMYJie2WmIHHzd4F6NCCLQ{WwQVI1KG6PLh?= MlW3NlEyPTV4MEW=
Ba/F3 cells NGCzZ2tHfW6ldHnvckBie3OjeR?= MkfDOlAhdWmwcx?= MkHETY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiSlHLNUBmgHC{ZYPz[YQhcW5iQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgOlAhdWmwczDifUBCdHCqYWPjdoVmdiCjc4PhfUwhUUN3ME2yOkBvVS5? NIrsNngzOjB6N{e1NC=>
human T cells NFf3eGRHfW6ldHnvckBie3OjeR?= M2DlfGlvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;u89yNKEmFNUC9Nlghdk1w M2W3[lI{PTRyNkS4
human PBMC NXnW[JFJTnWwY4Tpc44h[XO|YYm= MX2zNEBucW6| M3rnOWlvcGmkaYTpc44hd2ZiSlHLNU9LSUt|IHnuJIh2dWGwIGDCUWMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDJvc4TpcZVt[XSnZDDTWGFVeyCyaH;zdIhwenmuYYTpc44heHKnaX7jeYJifGWmIH\vdkA{OCCvaX7zJJBzcW:{IITvJGlNOiClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhOTVibXnud{BjgSCrboTyZYNmdGy3bHHyJJBpd3OobH;3JJN1[WmwaX7nMEBKSzVyPUOzJI5ONg>? M4nnO|IzODh5N{Ww
human TF1 cells NVTkcoRETnWwY4Tpc44h[XO|YYm= M{LpflIxKG2rboO= MV3Jcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWw3NWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHnuZ5Vj[XSnZDDmc5IhOjBibXnud{Bnd2yub4fl[EBjgSCLTE[gZ4hidGynbnflJIZweiB|MDDtbY5{KGmwIIDy[ZNmdmOnIH;mJJdpd2ynIHLsc49l97zOIFXDOVA:PDNibl2u NH\3bmQzOzZ3OUKxOC=>
mouse CTLL cells Mn;DSpVv[3Srb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKEqja{OtcYVlcWG2ZXSgTWwzNWmwZIXj[YQhW3SjdEWgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIFPUUGwh[2WubIOgZpkh[2WubD3iZZNm\CCjc4PhfUwhUUN3ME20PEBvVS5? NXPYW3A{OjFzNUW2NFU>
Ba/F3 cells MknHSpVv[3Srb36gZZN{[Xl? NGXnbIw3OCCvaX7z M3vzbWlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIFrBT|Mh\XiycnXzd4VlKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFYxKG2rboOgZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUC9OVQhdk1w NEXo[5ozOjB6N{e1NC=>
monkey T cells NFG4eGpHfW6ldHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGGubH;n[Y5q[yClZXzsd{1{fGmvdXzheIVlKHC{b3zp[oVz[XSrb36gbY4hdW:wa3X5JHQh[2WubIOgZpkhdWm6ZXSgcJlueGixY4n0[UBz\WGldHnvckBu\XSqb3SsJGlEPTB;NUegcm0v NHvzS|AyPDV7M{G4Ni=>
human monocytes M{K5eWZ2dmO2aX;uJIF{e2G7 MnvBTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJI1wdm:leYTld{BmgHC{ZYPzbY5oKEOGMUSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0Zvc4TpcZVt[XSnZDDTWGFVPWFicHjvd5Bpd3K7bHH0bY9vNCCLQ{WwQVAvOTh2IN88UU4> NEnrVIwzOzV2ME[0PC=>
human HUO3 cells NEjLPG9HfW6ldHnvckBie3OjeR?= M1e4[lQh\GG7cx?= NWfDXll{UW6qaXLpeIlwdiCxZjDoeY1idiCJTT3DV2YucW6mdXPl[EBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjVU|Mh[2WubIOgZZN{\XO|ZXSgZZMhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGGodHXyJFQh\GG7czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwM{K0JO69VS5? M{\EZVE1PTl|MUiy
mouse BAF3 cells MkXUVJJwdGmoZYLheIlwdiCjc4PhfS=> NWnvOZFIPzJiaB?= MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiZYjwdoV{e2mwZzDUSWwuUkGNMzDrbY5ie2ViYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVAvPTdizszNMi=> NFPNOHAyQTd4MkKzPC=>
human NK92 cells NFrCeYdHfW6ldHnvckBie3OjeR?= Mmr5NlAhdWmwcx?= M3jhbmlvcGmkaYTpc44hd2ZiVGnLNkBqdiCqdX3hckBPUzl{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxzMj3pcoR2[2WmIGPURXQ1KHCqb4PwbI9zgWyjdHnvckBqdmO3YnH0[YQh\m:{IEKwJI1qdnNiZn;scI94\WRiYomgTWwyOiClaHHscIVv\2ViZn;yJFQ2KG2rboOsJGVEPTB;MD63NUDPxE1w NImxbnkzOzZ3OUKxOC=>
TF1 cells MUHGeY5kfGmxbjDhd5NigQ>? M4foNGlvcGmkaYTpc44hd2ZiSVyzMYlv\HWlZXSgdJJwdGmoZYLheIlwdiCxZjDUSlEh[2WubIRvwKwhUUN3ME2wMlgh|ryPLh?= NHPsOI4yPjl|NES1Oy=>
human Jurkat cells Mny3SpVv[3Srb36gZZN{[Xl? M3fM[FI1KGh? NX\tTmFJUW6qaXLpeIlwdiCxZjDhcpRqNUOGMz;hcpRqNUOGMkitbY5lfWOnZDDJUFIheHKxZIXjeIlwdiCrbjDoeY1idiCMdYLrZZQh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUC9O{45PCEQvF2u NIj1W4MyPDV7M{G4Ni=>
human TALL-1 cells MkHpSpVv[3Srb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKEqDS{OgbY4hcHWvYX6gWGFNVC1zIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxvMjDpcoR2[2WmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBifCBzIIXNJJBz\WmwY4XiZZRm\CCob4KgN{BpenNiZn;scI94\WRiYomgTWwuOiCrbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCrbX31co9jdG:2dHnu[y=> MVGyOlI2QDV{MR?=
human DND/L12 cells NF\E[IxHfW6ldHnvckBie3OjeR?= MYKzNEBucW6| NXTMRmdKUW6qaXLpeIlwdiCxZjDKRWs{KGmwIHj1cYFvKESQRD;MNVIh[2WubIOgZYZ1\XJiM{CgcYlveyCkeTDseYNq\mW{YYPlJIF{e2G7IHnuJJBz\XOnbnPlJI9nKGi3bXHuJJNmenWvIHHsZpVucW5w M2fUelE1PTl|MUiy
human YT cells MX3GeY5kfGmxbjDhd5NigQ>? MlzzN|AhdmdxbXy= NGHyUWxKdmirYnn0bY9vKG:oIFnMNk1qdmS3Y3XkJGpCUzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFmWIHPlcIx{KGG2IEOwJI5oN22uIHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MUmxOFU6OzF6Mh?=
human OCL-AML5 cells MUfGeY5kfGmxbjDhd5NigQ>? NXPaUI1COSEQvF2= M1HjdFMhcA>? Mm[0TY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJG9EVC2DTVy1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiR12tR3NHKGmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIHH0JFEhfU1icILlbY5kfWKjdHXkJIZweiB|IHjyd{Bnd2yub4fl[EBjgSCJTT3DV2YhcW6mdXP0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhcW2vdX7vZoxwfHSrbne= MmPZNlYzPTh3MkG=
human CD4+ T cells Ml7KSpVv[3Srb36gZZN{[Xl? M{jhTlUhfG9iNUCwJI5O NWfzc3pFOSCq NUjFW|N1UW6qaXLpeIlwdiCxZjDJUFIucW6mdXPl[EBUfGG2NTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQ1S0L{BVKGOnbHzzJIF1KDVidH:gOVAxKG6PIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2 M{LId|E6ODV|N{W2
human Huh7 cells NXPDO5ZsTnWwY4Tpc44h[XO|YYm= NVXMOFd3OTBizszN MmTVN|AhdWmwcx?= NUPaSGZpUW6qaXLpeIlwdiCxZjDUfYszKGmwIHj1cYFvKEi3aEegZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEmITnHsdIhiPS2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDwdoUucW6ldXLheIVlKG[xcjCzNEBucW6|IHLl[o9z\SCLRl7hcJBp[TVic4TpcZVt[XSrb36g[o9zKDNyIH3pcpMhdWmwczDifUBqdW23bn;icI91fGmwZx?= M3LESlI3OjNzMUW5
human Hs578T cells M3zQRmZ2dmO2aX;uJIF{e2G7 M2PSOVMh|ryP M1y1cFE3KGh? NVi4fWFjUW6mdXP0bY9vKG:oIGDUVG43KGmwIHj1cYFvKEi|NUe4WEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCB|IIXNJIFnfGW{IEG2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKHCnco\hcoFl[XSn NFrIfVEzPDl5OEGxNi=>
human SUM149PT cells MYDGeY5kfGmxbjDhd5NigQ>? MWOzJO69VQ>? MY[xOkBp M4THW2lv\HWldHnvckBw\iCSVGDOOkBqdiCqdX3hckBUXU1zNEnQWEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCB|IIXNJIFnfGW{IEG2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKHCnco\hcoFl[XSn MXKyOFk4QDFzMh?=
human Huh7 cells MmTYSpVv[3Srb36gZZN{[Xl? MXqxNEDPxE1? M3HmclMxKG2rboO= NIH5dm5KdmirYnn0bY9vKG:oIGT5b|IhcW5iaIXtZY4hUHWqNzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[mG|YXygcIV3\WxiU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KDFyIIXNJIFnfGW{IEOwJI1qdnNiYomgbY1ufW6xYnzveJRqdmd? NXnHN4NOOjZ{M{GxOVk>
human UT7 cells MoDCSpVv[3Srb36gZZN{[Xl? MYDJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWXQ4KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGVRVy2|dHnteYxifGWmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBjgSCDbIDoZXNkemWnbjDhd5NigQ>? Mn;nNlY{PzJ4NUO=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[2]

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  • Cell lines: FDCP-EpoR JAK2WT and JAK2V617F cell lines
  • Concentrations: 0-4 μM
  • Incubation Time: 72 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[2]

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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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (198.21 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 504.49
Formula

C16H20N6O.C6H8O7

CAS No. 540737-29-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03502616 Recruiting Ankylosing Spondylitis Pfizer June 7 2018 Phase 3
NCT00413699 Completed Arthritis Rheumatoid Pfizer February 5 2007 Phase 3
NCT03159936 Recruiting Discoid Lupus Erythematosus|Systemic Lupus Erythematosus Tufts Medical Center|Pfizer April 3 2017 Early Phase 1
NCT02535689 Completed Systemic Lupus Erythematosus National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Institutes of Health Clinical Center (CC) August 28 2015 Phase 1
NCT01932372 Active not recruiting Rheumatoid Arthritis Pfizer July 26 2013 --
NCT03288324 Recruiting Cutaneous Lupus|Systemic Lupus Erythematosus Children''s Hospital Medical Center Cincinnati|Pfizer August 23 2017 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    What is the difference between the two products (S5001, S2789)?

  • Answer:

    Tofacitinib (S2789) is the base form of Tofacitinib citrate (S5001). The biological activity of these two compound are same. S5001 is better than S2789 for Oral gavage.

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID