Tofacitinib (CP-690550) Citrate

Licensed by Pfizer Catalog No.S5001

Tofacitinib (CP-690550) Citrate Chemical Structure

Molecular Weight(MW): 504.49

Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

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Cited by 34 Publications

4 Customer Reviews

  • 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 (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.
Targets
JAK3 [1]
(Cell-free assay)
JAK2 [4]
(Cell-free assay)
JAK1 [4]
(Cell-free assay)
ROCK2 [4]
(Cell-free assay)
LCK [4]
(Cell-free assay)
1 nM 20 nM 112 nM 3.4 μM 3.87 μM
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 NGXvVIhHfW6ldHnvckBie3OjeR?= MXSzNEBucW6| NGK3TWRKdmirYnn0bY9vKG:oIHj1cYFvKEeVVD3meZNm\CCMQVuzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmPUBk\WyuczD1d4lv\yCyb3z5[4x2fGGvaXOgZYNq\C22eYLvd4lv\SCjczDzeYJ{fHKjdHWgZYZ1\XJiM{CgcYlveyCkeTDFUGlUSSxiS3m9NE41KG6PLh?= MlvaNlM3Pjh2OES=
Sf9 cells MoXQSpVv[3Srb36gZZN{[Xl? NE\1c406OCCvaX7z MXvJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KE5vdHXycYlv[WxiR2PUMZRi\2enZDDKRWs{KGW6cILld5Nm\CCrbjDT[lkh[2WubIOgeZNqdmdiQnnveIlvNUyFLVXRSWRGWEWJRGnGSXdNTSCjczDzeYJ{fHKjdHWgZYZ1\XJiOUCgcYlveyCkeTDUVk1HWkWWIHHzd4F6NCCLQ{WwQVAvPiCwTT6= NYPWc3JtOjJyOEe3OVA>
SF21 cells NH7mSlVHfW6ldHnvckBie3OjeR?= NF\KR2syOCCvaX7z MYLJcohq[mm2aX;uJI9nKEqDS{KgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hW0Z{MTDj[YxteyC3c3nu[{BDcW:2aX6tT2FKTVSGS1XZXXRXU0RiYYOgd5Vje3S{YYTlJIFv\CCdM{PQ[4FudWGfQWTQJIlv[3WkYYTl[EBnd3JiMUCgcYlveyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCWb4Djc5VvfCCjbnHsfZNqeyxiSVO1NF01KG6PLh?= MU[yN|U1OTZ5MB?=
human MO7 cells NIHteFhHfW6ldHnvckBie3OjeR?= MWPJcohq[mm2aX;uJI9nKEqja{OtcYVlcWG2ZXSgTWwyPS2rbnT1Z4VlKFO2YYS1JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNU|ch[2WubIOgZpkh[2WubD3iZZNm\CCjc4PhfUwhUUN3ME2yOEBvVS5? Mmi3NlEyPTV4MEW=
Ba/F3 cells NFjScmFHfW6ldHnvckBie3OjeR?= Mk[2OlAhdWmwcx?= MYLJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCMQVuxJIV5eHKnc4Pl[EBqdiCEYT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBi\nSncjC2NEBucW6|IHL5JGFteGijU3Py[YVvKGG|c3H5MEBKSzVyPUK2JI5ONg>? Mo\zNlIxQDd5NUC=
human T cells NI[1fmFHfW6ldHnvckBie3OjeR?= NHG5WWJKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvcw+9lCCLQ{WwQVI5KG6PLh?= MXiyN|U1ODZ2OB?=
human PBMC MkLQSpVv[3Srb36gZZN{[Xl? NX\jfGN1OzBibXnudy=> NYPMRVFLUW6qaXLpeIlwdiCxZjDKRWsyN0qDS{OgbY4hcHWvYX6gVGJOSyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmOMj3zeIlufWyjdHXkJHNVSVS|IIDoc5NxcG:{eXzheIlwdiCycnXpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8hUUx{IHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiBzNTDtbY5{KGK7IHnueJJi[2WubIXsZZIheGixc3\sc5che3SjaX7pcoctKEmFNUC9N|Mhdk1w NX[5R4JnOjJyOEe3OVA>
human TF1 cells MYXGeY5kfGmxbjDhd5NigQ>? NUHjfYtoOjBibXnudy=> NHLXeZNKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkCgcYlveyCob3zsc5dm\CCkeTDJUFYh[2ijbHzlcodmKG[xcjCzNEBucW6|IHnuJJBz\XOnbnPlJI9nKHeqb3zlJIJtd2:m78{MJGVEPTB;NEOgcm0v MmHpNlM3PTl{MUS=
mouse CTLL cells NV3ab|h5TnWwY4Tpc44h[XO|YYm= NXWwVpYyUW6qaXLpeIlwdiCxZjDKZYs{NW2nZHnheIVlKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBEXEyOIHPlcIx{KGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVA:PDhibl2u MljINlEyPTV4MEW=
Ba/F3 cells M4nFSmZ2dmO2aX;uJIF{e2G7 MXW2NEBucW6| M1TGfGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIFrBT|Mh\XiycnXzd4VlKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFYxKG2rboOgZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUC9OVQhdk1w M33kdFIzODh5N{Ww
monkey T cells MoLlSpVv[3Srb36gZZN{[Xl? M4S1PWlvcGmkaYTpc44hd2ZiYXzsc4dmdmmlIHPlcIx{NXO2aX31cIF1\WRicILvcIln\XKjdHnvckBqdiCvb37r[ZkhXCClZXzsd{BjgSCvaYjl[EBtgW2yaH;jfZRmKHKnYXP0bY9vKG2ndHjv[EwhUUN3ME21O{BvVS5? MmLjNVQ2QTNzOEK=
human monocytes MmL1SpVv[3Srb36gZZN{[Xl? M2XscmlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OILYP0bY12dGG2ZXSgV3RCXDWjIIDoc5NxcG:{eXzheIlwdixiSVO1NF0xNjF6NDFOwG0v M{O0[VI{PTRyNkS4
human HUO3 cells NEfxeVlHfW6ldHnvckBie3OjeR?= M1nPVlQh\GG7cx?= NYPEbGZuUW6qaXLpeIlwdiCxZjDoeY1idiCJTT3DV2YucW6mdXPl[EBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjVU|Mh[2WubIOgZZN{\XO|ZXSgZZMhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGGodHXyJFQh\GG7czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwM{K0JO69VS5? M3;melE1PTl|MUiy
mouse BAF3 cells NEj5fGtRem:uaX\ldoF1cW:wIHHzd4F6 M{DSelczKGh? M1mxXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDlfJBz\XO|aX7nJHRGVC2MQVuzJItqdmG|ZTDh[pRmeiB5MjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC53NzFOwG0v MWqxPVc3OjJ|OB?=
human NK92 cells NFPKXnNHfW6ldHnvckBie3OjeR?= M2PxZVIxKG2rboO= M{LvNmlvcGmkaYTpc44hd2ZiVGnLNkBqdiCqdX3hckBPUzl{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxzMj3pcoR2[2WmIGPURXQ1KHCqb4PwbI9zgWyjdHnvckBqdmO3YnH0[YQh\m:{IEKwJI1qdnNiZn;scI94\WRiYomgTWwyOiClaHHscIVv\2ViZn;yJFQ2KG2rboOsJGVEPTB;MD63NUDPxE1w MkeyNlM3PTl{MUS=
TF1 cells NHTzZ2JHfW6ldHnvckBie3OjeR?= NWTMcFlpUW6qaXLpeIlwdiCxZjDJUFMucW6mdXPl[EBxem:uaX\ldoF1cW:wIH;mJHRHOSClZXzsd-+9lCCLQ{WwQVAvQCEQvF2u MkS1NVY6OzR2NUe=
human Jurkat cells Mlr4SpVv[3Srb36gZZN{[Xl? NVP0bW57OjRiaB?= MlHVTY5pcWKrdHnvckBw\iCjboTpMWNFOy:jboTpMWNFOjhvaX7keYNm\CCLTEKgdJJw\HWldHnvckBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTB;Nz64OEDPxE1w M4iyXlE1PTl|MUiy
human TALL-1 cells NGrpOXZHfW6ldHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKEqDS{OgbY4hcHWvYX6gWGFNVC1zIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxvMjDpcoR2[2WmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBifCBzIIXNJJBz\WmwY4XiZZRm\CCob4KgN{BpenNiZn;scI94\WRiYomgTWwuOiCrbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCrbX31co9jdG:2dHnu[y=> Mmm2NlYzPTh3MkG=
human DND/L12 cells MnjRSpVv[3Srb36gZZN{[Xl? NEfNO3A{OCCvaX7z MUnJcohq[mm2aX;uJI9nKEqDS{OgbY4hcHWvYX6gSG5FN0xzMjDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KGy3Y3nm[ZJie2ViYYPzZZkhcW5icILld4Vv[2Vib3[gbJVu[W5ic3XyeY0h[WykdX3pck4> NWfIdIZSOTR3OUOxPFI>
human YT cells MXLGeY5kfGmxbjDhd5NigQ>? NI\wRlY{OCCwZz;tcC=> NXT5WVY4UW6qaXLpeIlwdiCxZjDJUFIucW6mdXPl[EBLSUt|IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiC\VDDj[YxteyCjdDCzNEBv\y:vbDDifUBqdW23bn;icI91fGmwZzDhcoFtgXOrcx?= NV63dnMyOTR3OUOxPFI>
human OCL-AML5 cells MY\GeY5kfGmxbjDhd5NigQ>? M2nL[VEh|ryP MlnNN{Bp NHPGTllKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hV0OOLVHNUFUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0ZiaX7keYNm\CCVVFHUOUBxcG:|cHjvdplt[XSrb36gZZQhOSC3TTDwdoVqdmO3YnH0[YQh\m:{IEOgbJJ{KG[xbHzve4VlKGK7IFfNMWNUTiCrbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCrbX31co9jdG:2dHnu[y=> MU[yOlI2QDV{MR?=
human CD4+ T cells MnuySpVv[3Srb36gZZN{[Xl? M2nCVlUhfG9iNUCwJI5O NGPZW5YyKGh? NX;ofVgxUW6qaXLpeIlwdiCxZjDJUFIucW6mdXPl[EBUfGG2NTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQ1S0L{BVKGOnbHzzJIF1KDVidH:gOVAxKG6PIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2 MV6xPVA2Ozd3Nh?=
human Huh7 cells M1LTN2Z2dmO2aX;uJIF{e2G7 Mmj5NVAh|ryP NXn2UIVGOzBibXnudy=> MnjoTY5pcWKrdHnvckBw\iCWeXuyJIlvKGi3bXHuJGh2cDdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGlHVmGucHjhOU1qdmS3Y3XkJHNVSVR|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCycnWtbY5kfWKjdHXkJIZweiB|MDDtbY5{KGKnZn;y[UBKTk6jbIDoZVUhe3SrbYXsZZRqd25iZn;yJFMxKG2rboOgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? MV:yOlI{OTF3OR?=
human Hs578T cells NWfuSJBqTnWwY4Tpc44h[XO|YYm= NYPsN3pmOyEQvF2= NEDCOWwyPiCq NXXCXlRjUW6mdXP0bY9vKG:oIGDUVG43KGmwIHj1cYFvKEi|NUe4WEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCB|IIXNJIFnfGW{IEG2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKHCnco\hcoFl[XSn NITYe5czPDl5OEGxNi=>
human SUM149PT cells NEf3[2lHfW6ldHnvckBie3OjeR?= MlXhN{DPxE1? M3ztOlE3KGh? M{TZS2lv\HWldHnvckBw\iCSVGDOOkBqdiCqdX3hckBUXU1zNEnQWEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCB|IIXNJIFnfGW{IEG2JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKHCnco\hcoFl[XSn NFTQOZAzPDl5OEGxNi=>
human Huh7 cells NWTLU41WTnWwY4Tpc44h[XO|YYm= MXqxNEDPxE1? NHnUeVg{OCCvaX7z M{D5SmlvcGmkaYTpc44hd2ZiVInrNkBqdiCqdX3hckBJfWh5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBj[XOjbDDs[ZZmdCCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZYZ1\XJiM{CgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? MojWNlYzOzFzNUm=
human UT7 cells MlS4SpVv[3Srb36gZZN{[Xl? NGryXZdKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXVR5IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEWSTz3zeIlufWyjdHXkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCkeTDBcJBp[VOlcnXlckBie3OjeR?= NV7YVY54OjZ|N{K2OVM>

... 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]
+ Expand

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 <1 mg/mL
Ethanol <1 mg/mL
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.

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
NCT02535689 Recruiting Systemic Lupus Erythematosus National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)|National Institutes of Health Clinical Center (CC) August 25, 2015 Phase 1
NCT03000439 Not yet recruiting Arthritis Juvenile Idiopathic Pfizer April 2017 Phase 3
NCT03002649 Recruiting Dermatomyositis Johns Hopkins University|Pfizer January 2017 Phase 1
NCT03011281 Recruiting Rheumatoid Arthritis Hanyang University November 2016 --
NCT02996500 Recruiting Rheumatoid Arthritis Pfizer November 2016 Phase 2
NCT02812342 Active, not recruiting Alopecia Areata|Alopecia Totalis|Alopecia Universalis Yale University September 2016 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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