Tofacitinib (CP-690550) Citrate

Licensed by Pfizer 製品コードS5001

Tofacitinib (CP-690550) Citrate化学構造

分子量(MW):504.49

Tofacitinib (CP-690550) Citrateは一種の新たなJAK3阻害剤で、無細胞試験でIC50値が1 nMになって、JAK3に作用する選択性はJAK2とJAK1に作用する選択性より20-100倍が高くなります。

サイズ 価格 在庫  
JPY 27516.10 あり
JPY 21166.23 あり
JPY 67674.36 あり

文献中の引用(34)

カスタマーフィードバック(4)

  • 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.

製品安全説明書

JAK阻害剤の選択性比較

生物活性

製品説明 Tofacitinib (CP-690550) Citrateは一種の新たなJAK3阻害剤で、無細胞試験でIC50値が1 nMになって、JAK3に作用する選択性はJAK2とJAK1に作用する選択性より20-100倍が高くなります。
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NIjYXVhHfW6ldHnvckBie3OjeR?= MkP1N|AhdWmwcx?= MknqTY5pcWKrdHnvckBw\iCqdX3hckBIW1RvZoXz[YQhUkGNMzDjZZRidHm2aXOg[I9u[WmwIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkmgZ4VtdHNidYPpcocheG:ueXfseZRidWmlIHHjbYQufHm{b4PpcoUh[XNic4Xid5Rz[XSnIHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEurPUCuOEBvVS5? NHnnU|UzOzZ4OES4OC=>
Sf9 cells MVfGeY5kfGmxbjDhd5NigQ>? M3jH[lkxKG2rboO= NVTJVWxZUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJGdUXC22YXfn[YQhUkGNMzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGJqd3Srbj3MR{1GWUWGRWDFS2R[TkWZTFWgZZMhe3Wkc4TyZZRmKGGodHXyJFkxKG2rboOgZpkhXFJvRmLFWEBie3OjeTygTWM2OD1yLk[gcm0v MmPHNlIxQDd5NUC=
SF21 cells M4nrRWZ2dmO2aX;uJIF{e2G7 NGHEblcyOCCvaX7z NF[zWmdKdmirYnn0bY9vKG:oIFrBT|IhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iU1[yNUBk\WyuczD1d4lv\yCEaX;0bY4uU0GLRWTET2V[YVSYS1SgZZMhe3Wkc4TyZZRmKGGwZDDbN|NR\2GvbXHdRXRRKGmwY4XiZZRm\CCob4KgNVAhdWmwczDwdolweiC2bzDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiM{CgcYlveyCkeTDUc5Bkd3WwdDDhcoFtgXOrczygTWM2OD12IH7NMi=> M17HWVI{PTRzNkew
human MO7 cells M1zHTGZ2dmO2aX;uJIF{e2G7 NE\SR|JKdmirYnn0bY9vKG:oIFrhb|MudWWmaXH0[YQhUUxzNT3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBOVzdiY3XscJMh[nliY3XscE1j[XOnZDDhd5NigSxiSVO1NF0zPCCwTT6= Mkm0NlEyPTV4MEW=
Ba/F3 cells Mkn3SpVv[3Srb36gZZN{[Xl? MXO2NEBucW6| M1PNeGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIFrBT|Eh\XiycnXzd4VlKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFYxKG2rboOgZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUC9NlYhdk1w NFqw[4ozOjB6N{e1NC=>
human T cells NUGweYtRTnWwY4Tpc44h[XO|YYm= MlzVTY5pcWKrdHnvckBw\iCMQVuzM|EhcW5iaIXtZY4hXCClZXzsd{BmgHC{ZYPzbY5oKEOGMzDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMNk1{fGmvdXzheIVlKFOWQWS1ZUBxcG:|cHjvdplt[XSrb39vwKwhUUN3ME2yPEBvVS5? MVyyN|U1ODZ2OB?=
human PBMC MofSSpVv[3Srb36gZZN{[Xl? NUOwSnFvOzBibXnudy=> NYPXT2M4UW6qaXLpeIlwdiCxZjDKRWsyN0qDS{OgbY4hcHWvYX6gVGJOSyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmOMj3zeIlufWyjdHXkJHNVSVS|IIDoc5NxcG:{eXzheIlwdiCycnXpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8hUUx{IHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiBzNTDtbY5{KGK7IHnueJJi[2WubIXsZZIheGixc3\sc5che3SjaX7pcoctKEmFNUC9N|Mhdk1w NX\BfZlEOjJyOEe3OVA>
human TF1 cells NGryfYpHfW6ldHnvckBie3OjeR?= M1nFU|IxKG2rboO= MnXJTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDpcoN2[mG2ZXSg[o9zKDJyIH3pcpMh\m:ubH;3[YQh[nliSVy2JINp[WyuZX7n[UBnd3JiM{CgcYlveyCrbjDwdoV{\W6lZTDv[kB4cG:uZTDicI9w\O,:jDDFR|UxRTR|IH7NMi=> NXWzPZZVOjN4NUmyNVQ>
mouse CTLL cells NHvBPWtHfW6ldHnvckBie3OjeR?= M33GNmlvcGmkaYTpc44hd2ZiSnHrN{1u\WSrYYTl[EBKVDJvaX7keYNm\CCVdHH0OUBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgR3RNVCClZXzsd{BjgSClZXzsMYJie2WmIHHzd4F6NCCLQ{WwQVQ5KG6PLh?= NXvieIlTOjFzNUW2NFU>
Ba/F3 cells M2PTT2Z2dmO2aX;uJIF{e2G7 NWrZNI5GPjBibXnudy=> MnvyTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiSlHLN{BmgHC{ZYPz[YQhcW5iQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgOlAhdWmwczDifUBCdHCqYWPjdoVmdiCjc4PhfUwhUUN3ME21OEBvVS5? NFz3TJYzOjB6N{e1NC=>
monkey T cells NGXw[VlHfW6ldHnvckBie3OjeR?= NXS0dGFrUW6qaXLpeIlwdiCxZjDhcIxw\2WwaXOgZ4VtdHNvc4TpcZVt[XSnZDDwdo9tcW[ncnH0bY9vKGmwIH3vcotmgSCWIHPlcIx{KGK7IH3pfIVlKGy7bYDoc4N6fGVicnXhZ5Rqd25ibXX0bI9lNCCLQ{WwQVU4KG6PLh?= MVexOFU6OzF6Mh?=
human monocytes M2LGSWZ2dmO2aX;uJIF{e2G7 MomxTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJI1wdm:leYTld{BmgHC{ZYPzbY5oKEOGMUSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0Zvc4TpcZVt[XSnZDDTWGFVPWFicHjvd5Bpd3K7bHH0bY9vNCCLQ{WwQVAvOTh2IN88UU4> M1X2UlI{PTRyNkS4
human HUO3 cells NVfOeFVwTnWwY4Tpc44h[XO|YYm= M1TPVFQh\GG7cx?= MkHNTY5pcWKrdHnvckBw\iCqdX3hckBIVS2FU1[tbY5lfWOnZDDwdo9tcW[ncnH0bY9vKGmwIHj1cYFvKEiXT{OgZ4VtdHNiYYPz[ZN{\WRiYYOgX|NJZXSqeX3p[Ilv\SCrbnPvdpBwemG2aX;uJIFnfGW{IESg[IF6eyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvOzJ2IN88UU4> NUfE[2I1OTR3OUOxPFI>
mouse BAF3 cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 M4ryUVczKGh? MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiZYjwdoV{e2mwZzDUSWwuUkGNMzDrbY5ie2ViYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVAvPTdizszNMi=> MoXINVk4PjJ{M{i=
human NK92 cells M3;JR2Z2dmO2aX;uJIF{e2G7 MWKyNEBucW6| NW\vOoFxUW6qaXLpeIlwdiCxZjDUXWszKGmwIHj1cYFvKE6NOUKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCLTEGyMYlv\HWlZXSgV3RCXDRicHjvd5Bpd3K7bHH0bY9vKGmwY4XiZZRm\CCob4KgNlAhdWmwczDmc4xtd3enZDDifUBKVDF{IHPoZYxt\W6pZTDmc5IhPDVibXnud{whTUN3ME2wMlcyKM7:TT6= MnXhNlM3PTl{MUS=
TF1 cells MknzSpVv[3Srb36gZZN{[Xl? NIj5TnFKdmirYnn0bY9vKG:oIFnMN{1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gWGYyKGOnbHzz89yNKEmFNUC9NE45KM7:TT6= NELWZ|IyPjl|NES1Oy=>
human Jurkat cells NH6yO|dHfW6ldHnvckBie3OjeR?= NHnyd2EzPCCq MV\Jcohq[mm2aX;uJI9nKGGwdHmtR2Q{N2GwdHmtR2QzQC2rbnT1Z4VlKEmOMjDwdo9lfWO2aX;uJIlvKGi3bXHuJGp2emujdDDj[YxteyCjZoTldkAzPCCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OD15Lki0JO69VS5? MkTCNVQ2QTNzOEK=
human TALL-1 cells MWfGeY5kfGmxbjDhd5NigQ>? M4e3T2lvcGmkaYTpc44hd2ZiSlHLN{BqdiCqdX3hckBVSUyOLUGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCLTD2yJIlv\HWlZXSgV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGG2IEGgeW0heHKnaX7jeYJifGWmIH\vdkA{KGi{czDmc4xtd3enZDDifUBKVC1{IHnu[JVkfGmxbjDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGK7IHntcZVvd2Kub4T0bY5o M2L0RlI3OjV6NUKx
human DND/L12 cells MYrGeY5kfGmxbjDhd5NigQ>? M1rzdlMxKG2rboO= NYTUbZNwUW6qaXLpeIlwdiCxZjDKRWs{KGmwIHj1cYFvKESQRD;MNVIh[2WubIOgZYZ1\XJiM{CgcYlveyCkeTDseYNq\mW{YYPlJIF{e2G7IHnuJJBz\XOnbnPlJI9nKGi3bXHuJJNmenWvIHHsZpVucW5w NFHvNlcyPDV7M{G4Ni=>
human YT cells M{e2VmZ2dmO2aX;uJIF{e2G7 NV64NYl6OzBibnevcYw> NH65PIxKdmirYnn0bY9vKG:oIFnMNk1qdmS3Y3XkJGpCUzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFmWIHPlcIx{KGG2IEOwJI5oN22uIHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| MoLONVQ2QTNzOEK=
human OCL-AML5 cells M2rLWWZ2dmO2aX;uJIF{e2G7 MWixJO69VQ>? Mn;rN{Bp MmPqTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJG9EVC2DTVy1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiR12tR3NHKGmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIHH0JFEhfU1icILlbY5kfWKjdHXkJIZweiB|IHjyd{Bnd2yub4fl[EBjgSCJTT3DV2YhcW6mdXP0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhcW2vdX7vZoxwfHSrbne= NIDTU|AzPjJ3OEWyNS=>
human CD4+ T cells Mnr0SpVv[3Srb36gZZN{[Xl? Ml\IOUB1dyB3MECgcm0> MUCxJIg> M130XWlvcGmkaYTpc44hd2ZiSVyyMYlv\HWlZXSgV5RifDVicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEOGNDugWEBk\WyuczDheEA2KHSxIEWwNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfA>? NYrhOm5JOTlyNUO3OVY>
human Huh7 cells MonRSpVv[3Srb36gZZN{[Xl? Mor2NVAh|ryP Mo\RN|AhdWmwcx?= NHrPSoxKdmirYnn0bY9vKG:oIGT5b|IhcW5iaIXtZY4hUHWqNzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhUU[QYXzwbIE2NWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JFExKHWPIIDy[U1qdmO3YnH0[YQh\m:{IEOwJI1qdnNiYnXmc5JmKEmITnHsdIhiPSC|dHnteYxifGmxbjDmc5IhOzBibXnud{BucW6|IHL5JIludXWwb3Lsc5R1cW6p MoHSNlYzOzFzNUm=
human Hs578T cells MYXGeY5kfGmxbjDhd5NigQ>? M3n5UlMh|ryP NXuzNHhXOTZiaB?= M1;GN2lv\HWldHnvckBw\iCSVGDOOkBqdiCqdX3hckBJezV5OGSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOyC3TTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBx\XK4YX7h[IF1\Q>? M2LzcVI1QTd6MUGy
human SUM149PT cells M3PI[mZ2dmO2aX;uJIF{e2G7 M1;Jc|Mh|ryP NXHEcZJwOTZiaB?= NIL4UHRKdmS3Y4Tpc44hd2ZiUGTQUlYhcW5iaIXtZY4hW1WPMUS5VHQh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiMzD1UUBi\nSncjCxOkBpenNiYomgW4V{fGW{bjDicI91fGmwZzDhcoFtgXOrczDpckBxemW|ZX7j[UBw\iCyZYL2ZY5i\GG2ZR?= MVWyOFk4QDFzMh?=
human Huh7 cells MWrGeY5kfGmxbjDhd5NigQ>? MlvvNVAh|ryP MlXnN|AhdWmwcx?= M3OwUmlvcGmkaYTpc44hd2ZiVInrNkBqdiCqdX3hckBJfWh5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBj[XOjbDDs[ZZmdCCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZYZ1\XJiM{CgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? NELpclMzPjJ|MUG1PS=>
human UT7 cells MVnGeY5kfGmxbjDhd5NigQ>? NIr6cIFKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXVR5IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEWSTz3zeIlufWyjdHXkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCkeTDBcJBp[VOlcnXlckBie3OjeR?= NWHVW|gzOjZ|N{K2OVM>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [2]
+ 展開
  • 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.
    (参考用のみ)
動物試験: [2]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (198.21 mM) warming
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
0.5% methylcellulose
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 504.49
化学式

C16H20N6O.C6H8O7

CAS No. 540737-29-9
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

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

  • 回答:

    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信号経路図

JAK Inhibitors with Unique Features

相関JAK製品

Tags: Tofacitinib (CP-690550) Citrateを買う | Tofacitinib (CP-690550) Citrate ic50 | Tofacitinib (CP-690550) Citrate供給者 | Tofacitinib (CP-690550) Citrateを購入する | Tofacitinib (CP-690550) Citrate費用 | Tofacitinib (CP-690550) Citrate生産者 | オーダーTofacitinib (CP-690550) Citrate | Tofacitinib (CP-690550) Citrate化学構造 | Tofacitinib (CP-690550) Citrate分子量 | Tofacitinib (CP-690550) Citrate代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID