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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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 NXX5O|hDTnWwY4Tpc44h[XO|YYm= NWDleYp4OzBibXnudy=> MUjJcohq[mm2aX;uJI9nKGi3bXHuJGdUXC2odYPl[EBLSUt|IHPheIFtgXSrYzDkc41icW5iZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{NWmwZnXjeIVlKFOoOTDj[YxteyC3c3nu[{Bxd2y7Z3z1eIFucWNiYXPp[E11gXKxc3nu[UBieyC|dXLzeJJifGViYX\0[ZIhOzBibXnud{BjgSCHTFnTRUwhU2l;MD60JI5ONg>? MmT0NlM3Pjh2OES=
Sf9 cells M4TaW2Z2dmO2aX;uJIF{e2G7 NGrCVI86OCCvaX7z NHzqeVdKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IF6teIVzdWmwYXygS3NVNXSjZ3fl[EBLSUt|IHX4dJJme3OnZDDpckBU\jliY3XscJMhfXOrbnegRolwfGmwLVzDMWVSTUSHUFXHSHlHTVeORTDhd{B{fWK|dILheIUh[W[2ZYKgPVAhdWmwczDifUBVWi2IUlXUJIF{e2G7LDDJR|UxRTBwNjDuUU4> NYHqfoxoOjJyOEe3OVA>
SF21 cells NF;Be4dHfW6ldHnvckBie3OjeR?= M2rRd|ExKG2rboO= MoPZTY5pcWKrdHnvckBw\iCMQVuyJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKFOIMkGgZ4VtdHNidYPpcochSmmxdHnuMWtCUUWWRFvFXXlVXkuGIHHzJJN2[nO2cnH0[UBidmRiW{OzVIdidW2jXVHUVEBqdmO3YnH0[YQh\m:{IEGwJI1qdnNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliVH;wZ492dnRiYX7hcJl{cXNuIFnDOVA:PCCwTT6= NGnr[ZEzOzV2MU[3NC=>
human MO7 cells MUTGeY5kfGmxbjDhd5NigQ>? NEHTfGtKdmirYnn0bY9vKG:oIFrhb|MudWWmaXH0[YQhUUxzNT3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOVzdiY3XscJMh[nliY3XscE1j[XOnZDDhd5NigSxiSVO1NF0zPCCwTT6= MXmyNVE2PTZyNR?=
Ba/F3 cells NGS2PFBHfW6ldHnvckBie3OjeR?= MYO2NEBucW6| NYSyZZdxUW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgTmFMOSCneIDy[ZN{\WRiaX6gRoEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBUXEGWNTDwbI9{eGixconsZZRqd25iYX\0[ZIhPjBibXnud{BjgSCDbIDoZXNkemWnbjDhd5NigSxiSVO1NF0zPiCwTT6= NUjHOnp4OjJyOEe3OVA>
human T cells NYS4fmN{TnWwY4Tpc44h[XO|YYm= NU[0THBDUW6qaXLpeIlwdiCxZjDKRWs{NzFiaX6gbJVu[W5iVDDj[YxteyCneIDy[ZN{cW6pIFPEN{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc47wxIxiSVO1NF0zQCCwTT6= MUmyN|U1ODZ2OB?=
human PBMC Mn7GSpVv[3Srb36gZZN{[Xl? MnLUN|AhdWmwcx?= NXT3OXZDUW6qaXLpeIlwdiCxZjDKRWsyN0qDS{OgbY4hcHWvYX6gVGJOSyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmOMj3zeIlufWyjdHXkJHNVSVS|IIDoc5NxcG:{eXzheIlwdiCycnXpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8hUUx{IHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiBzNTDtbY5{KGK7IHnueJJi[2WubIXsZZIheGixc3\sc5che3SjaX7pcoctKEmFNUC9N|Mhdk1w MonZNlIxQDd5NUC=
human TF1 cells M{T4cGZ2dmO2aX;uJIF{e2G7 MnXUNlAhdWmwcx?= M2TWZmlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gbY5kfWKjdHXkJIZweiB{MDDtbY5{KG[xbHzve4VlKGK7IFnMOkBkcGGubHXu[4Uh\m:{IEOwJI1qdnNiaX6gdJJme2WwY3Wgc4Yhf2ixbHWgZoxwd2UxvJygSWM2OD12MzDuUU4> NGPVU4QzOzZ3OUKxOC=>
mouse CTLL cells MnThSpVv[3Srb36gZZN{[Xl? NXe2[WRWUW6qaXLpeIlwdiCxZjDKZYs{NW2nZHnheIVlKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBEXEyOIHPlcIx{KGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVA:PDhibl2u NIfvNpczOTF3NU[wOS=>
Ba/F3 cells M{jKfmZ2dmO2aX;uJIF{e2G7 NGmzV283OCCvaX7z Ml7xTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiSlHLN{BmgHC{ZYPz[YQhcW5iQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgOlAhdWmwczDifUBCdHCqYWPjdoVmdiCjc4PhfUwhUUN3ME21OEBvVS5? NFyzSoYzOjB6N{e1NC=>
monkey T cells M4f2PGZ2dmO2aX;uJIF{e2G7 NGPKbotKdmirYnn0bY9vKG:oIHHscI9o\W6rYzDj[Yxtey2|dHnteYxifGWmIIDyc4xq\mW{YYTpc44hcW5ibX;ub4V6KFRiY3XscJMh[nlibXn4[YQhdHmvcHjvZ5l1\SC{ZXHjeIlwdiCvZYToc4QtKEmFNUC9OVchdk1w MYexOFU6OzF6Mh?=
human monocytes MVjGeY5kfGmxbjDhd5NigQ>? M2rCW2lvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OILYP0bY12dGG2ZXSgV3RCXDWjIIDoc5NxcG:{eXzheIlwdixiSVO1NF0xNjF6NDFOwG0v NU\QcnFsOjN3NEC2OFg>
human HUO3 cells NEHHUmhHfW6ldHnvckBie3OjeR?= MV20JIRigXN? NYnlbY9bUW6qaXLpeIlwdiCxZjDoeY1idiCJTT3DV2YucW6mdXPl[EBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjVU|Mh[2WubIOgZZN{\XO|ZXSgZZMhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGGodHXyJFQh\GG7czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwM{K0JO69VS5? NFL1b4oyPDV7M{G4Ni=>
mouse BAF3 cells NXzWN|NUWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVi4S|g{PzJiaB?= MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiZYjwdoV{e2mwZzDUSWwuUkGNMzDrbY5ie2ViYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVAvPTdizszNMi=> MWqxPVc3OjJ|OB?=
human NK92 cells NXHVbldxTnWwY4Tpc44h[XO|YYm= MlPPNlAhdWmwcx?= Ml;tTY5pcWKrdHnvckBw\iCWWVuyJIlvKGi3bXHuJG5MQTJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDF{LXnu[JVk\WRiU2TBWFQheGixc4Doc5J6dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkCgcYlveyCob3zsc5dm\CCkeTDJUFEzKGOqYXzs[Y5o\SCob4KgOFUhdWmwczygSWM2OD1yLkexJO69VS5? M2jnflI{PjV7MkG0
TF1 cells MmnHSpVv[3Srb36gZZN{[Xl? MVTJcohq[mm2aX;uJI9nKEmOMz3pcoR2[2WmIIDyc4xq\mW{YYTpc44hd2ZiVF[xJINmdGy|78{MJGlEPTB;MD64JO69VS5? MljDNVY6OzR2NUe=
human Jurkat cells NUG5e3hnTnWwY4Tpc44h[XO|YYm= NYrNS5RQOjRiaB?= M1HUU2lvcGmkaYTpc44hd2ZiYX70bU1ETDNxYX70bU1ETDJ6LXnu[JVk\WRiSVyyJJBzd2S3Y4Tpc44hcW5iaIXtZY4hUnW{a3H0JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUeuPFQh|ryPLh?= NUPRdmVyOTR3OUOxPFI>
human TALL-1 cells MY\GeY5kfGmxbjDhd5NigQ>? M4rRUGlvcGmkaYTpc44hd2ZiSlHLN{BqdiCqdX3hckBVSUyOLUGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCLTD2yJIlv\HWlZXSgV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGG2IEGgeW0heHKnaX7jeYJifGWmIH\vdkA{KGi{czDmc4xtd3enZDDifUBKVC1{IHnu[JVkfGmxbjDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IHntcZVvd2Kub4T0bY5o MoHZNlYzPTh3MkG=
human DND/L12 cells MXnGeY5kfGmxbjDhd5NigQ>? NVe4VnRpOzBibXnudy=> MoLBTY5pcWKrdHnvckBw\iCMQVuzJIlvKGi3bXHuJGRPTC:OMUKgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCudXPp[oVz[XOnIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJIh2dWGwIIPldpVuKGGuYoXtbY4v MWOxOFU6OzF6Mh?=
human YT cells M1zXd2Z2dmO2aX;uJIF{e2G7 M1jzS|MxKG6pL33s M1LWTGlvcGmkaYTpc44hd2ZiSVyyMYlv\HWlZXSgTmFMOyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hYVRiY3XscJMh[XRiM{CgcocwdWxiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? MlW5NVQ2QTNzOEK=
human OCL-AML5 cells MmTISpVv[3Srb36gZZN{[Xl? M{PtSVEh|ryP MVuzJIg> NWDHenZ5UW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKE:FTD3BUWw2KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OIIHnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJIF1KDFidV2gdJJmcW6ldXLheIVlKG[xcjCzJIhzeyCob3zsc5dm\CCkeTDHUU1EW0ZiaX7keYN1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliaX3teY5w[myxdITpcoc> NHfNZlkzPjJ3OEWyNS=>
human CD4+ T cells MWPGeY5kfGmxbjDhd5NigQ>? NI[2XJE2KHSxIEWwNEBvVQ>? MnjpNUBp MVzJcohq[mm2aX;uJI9nKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBETDRtIGSgZ4VtdHNiYYSgOUB1dyB3MECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Q> MXWxPVA2Ozd3Nh?=
human Huh7 cells MW\GeY5kfGmxbjDhd5NigQ>? NYDQZow1OTBizszN NUHMVY14OzBibXnudy=> MnHKTY5pcWKrdHnvckBw\iCWeXuyJIlvKGi3bXHuJGh2cDdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGlHVmGucHjhOU1qdmS3Y3XkJHNVSVR|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCycnWtbY5kfWKjdHXkJIZweiB|MDDtbY5{KGKnZn;y[UBKTk6jbIDoZVUhe3SrbYXsZZRqd25iZn;yJFMxKG2rboOgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? M1jsNlI3OjNzMUW5
human Hs578T cells Ml;FSpVv[3Srb36gZZN{[Xl? NHjNSHM{KM7:TR?= NEfKZnAyPiCq MknDTY5lfWO2aX;uJI9nKFCWUF62JIlvKGi3bXHuJGh{PTd6VDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEA{KHWPIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJJBmen[jbnHkZZRm NVrUTGk2OjR7N{ixNVI>
human SUM149PT cells MVzGeY5kfGmxbjDhd5NigQ>? NIWybmQ{KM7:TR?= M1nK[VE3KGh? NUnkcFJHUW6mdXP0bY9vKG:oIGDUVG43KGmwIHj1cYFvKFOXTUG0PXBVKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9vKGG2IEOgeW0h[W[2ZYKgNVYhcHK|IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYOgbY4heHKnc3XuZ4Uhd2ZicHXyeoFv[WSjdHW= Mn6xNlQ6PzhzMUK=
human Huh7 cells NV7pWm0{TnWwY4Tpc44h[XO|YYm= MV:xNEDPxE1? NWTscG1rOzBibXnudy=> NUL2ZXFGUW6qaXLpeIlwdiCxZjDUfYszKGmwIHj1cYFvKEi3aEegZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGKjc3HsJIxmfmWuIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCBzMDD1UUBi\nSncjCzNEBucW6|IHL5JIludXWwb3Lsc5R1cW6p MYGyOlI{OTF3OR?=
human UT7 cells MYHGeY5kfGmxbjDhd5NigQ>? M2HWWmlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBWXDdiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhTVCRLYP0bY12dGG2ZXSgV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGK7IFHsdIhiW2O{ZXXuJIF{e2G7 M4fNUlI3Ozd{NkWz

... 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
NCT03598959 Not yet recruiting Extranodal NK/T-cell Lymphoma Sichuan University January 1 2019 Phase 2
NCT03681275 Not yet recruiting Diaphragm Injury Stanford University December 1 2018 Phase 1
NCT03580343 Not yet recruiting Uveitis|Scleritis Washington University School of Medicine September 2018 Phase 2
NCT03486457 Recruiting Psoriatic Arthritis Pfizer August 10 2018 Phase 3
NCT03502616 Recruiting Ankylosing Spondylitis Pfizer June 7 2018 Phase 3
NCT03000439 Recruiting Arthritis Juvenile Idiopathic Pfizer May 10 2018 Phase 3

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.

  • * Indicates a Required Field

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