Tofacitinib (CP-690550) Citrate

Pfizer辉瑞授权 目录号:S5001

Tofacitinib (CP-690550) Citrate Chemical Structure

Molecular Weight(MW): 504.49

Tofacitinib (CP-690550) Citrate是一种新型JAK抑制剂,对JAK3,JAK2,JAK1的IC50分别为1 nM, 20 nM 和112 nM。

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RMB 1561.36 现货
RMB 1194.19 现货
RMB 3843.17 现货
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客户购买Selleck的此次产品后发表的文献34篇:

客户使用该产品的4个实验数据:

  • 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.

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Tofacitinib (CP-690550) Citrate是一种新型JAK抑制剂,对JAK3,JAK2,JAK1的IC50分别为1 nM, 20 nM 和112 nM。
靶点
JAK3 [1]
(Cell-free assay)
JAK2 [4]
(Cell-free assay)
1 nM 20 nM
体外研究

CP-690550抑制IL-2调节的人T细胞爆发式增殖,和IL-15诱导的CD69表达,IC50分别为11和48 nM。CP-690550抑制混合淋巴细胞反应,IC50为87 nM。CPCP-690550 处理含人野生型或V617F JAK2的鼠因子依赖的细胞Patersen–促红细胞生成素受体(FDCP-EpoR) 细胞,抑制细胞增殖,IC50分别为2.1 µM 和0.25 µM。CP-690550 抑制白细胞介素-6诱导的STAT1 和STAT3磷酸化,IC50分别为23和77 nM。而且, CP-690550作用于携带JAK2V617F的小鼠 FDCP-EpoR细胞,具有显著的促凋亡作用,然而效果比作用于携带野生型JAK2的细胞低。伴随着抑制关键JAK2V617F依赖的下游信号效应器信号转导的磷酸化,及(STAT)3, STAT5, 和v-akt小鼠胸腺瘤病毒癌基因同源(AKT)的转录激活。[2] 此外, CP-690550 在体外作用于人猕猴 NK 和CD8+ T 细胞,抑制IL-15诱导的CD69表达。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells NYexfIF{TnWwY4Tpc44h[XO|YYm= M1vYe|MxKG2rboO= M3zpcWlvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLX\1d4VlKEqDS{OgZ4F1[Wy7dHnjJIRwdWGrbjDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiU3[5JINmdGy|IIXzbY5oKHCxbInncJV1[W2rYzDhZ4llNXS7cn;zbY5mKGG|IIP1ZpN1emG2ZTDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCNaU2wMlQhdk1w NFH2N5MzOzZ4OES4OC=>
Sf9 cells MlP0SpVv[3Srb36gZZN{[Xl? M2LiNFkxKG2rboO= M3;YdWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiTj30[ZJucW6jbDDHV3QufGGpZ3XkJGpCUzNiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{B2e2mwZzDCbY91cW5vTFOtSXFGTEWSRVfEXWZGX0yHIHHzJJN2[nO2cnH0[UBi\nSncjC5NEBucW6|IHL5JHRTNU[URWSgZZN{[XluIFnDOVA:OC54IH7NMi=> NWrxNpkzOjJyOEe3OVA>
SF21 cells NVfhe2ZmTnWwY4Tpc44h[XO|YYm= MkS0NVAhdWmwcx?= NIDvSI9KdmirYnn0bY9vKG:oIFrBT|IhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iU1[yNUBk\WyuczD1d4lv\yCEaX;0bY4uU0GLRWTET2V[YVSYS1SgZZMhe3Wkc4TyZZRmKGGwZDDbN|NR\2GvbXHdRXRRKGmwY4XiZZRm\CCob4KgNVAhdWmwczDwdolweiC2bzDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiM{CgcYlveyCkeTDUc5Bkd3WwdDDhcoFtgXOrczygTWM2OD12IH7NMi=> NX35[WtiOjN3NEG2O|A>
human MO7 cells NW\M[mlNTnWwY4Tpc44h[XO|YYm= MlHxTY5pcWKrdHnvckBw\iCMYXuzMY1m\GmjdHXkJGlNOTVvaX7keYNm\CCVdHH0OUBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUW84KGOnbHzzJIJ6KGOnbHytZoF{\WRiYYPzZZktKEmFNUC9NlQhdk1w M{\NXFIyOTV3NkC1
Ba/F3 cells M3;3emZ2dmO2aX;uJIF{e2G7 NE\EbVI3OCCvaX7z M{LMSWlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIFrBT|Eh\XiycnXzd4VlKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFYxKG2rboOgZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUC9NlYhdk1w NWnQW4lJOjJyOEe3OVA>
human T cells NGnuVXRHfW6ldHnvckBie3OjeR?= MXrJcohq[mm2aX;uJI9nKEqDS{OvNUBqdiCqdX3hckBVKGOnbHzzJIV5eHKnc4PpcochS0R|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVyyMZN1cW23bHH0[YQhW1SDVEXhJJBpd3OyaH;yfYxifGmxbv-8kEBKSzVyPUK4JI5ONg>? NUTnSmNCOjN3NEC2OFg>
human PBMC MU\GeY5kfGmxbjDhd5NigQ>? NGLCb44{OCCvaX7z NU[0NmdFUW6qaXLpeIlwdiCxZjDKRWsyN0qDS{OgbY4hcHWvYX6gVGJOSyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmOMj3zeIlufWyjdHXkJHNVSVS|IIDoc5NxcG:{eXzheIlwdiCycnXpcoN2[mG2ZXSg[o9zKDNyIH3pcpMheHKrb4KgeI8hUUx{IHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiBzNTDtbY5{KGK7IHnueJJi[2WubIXsZZIheGixc3\sc5che3SjaX7pcoctKEmFNUC9N|Mhdk1w M1i2V|IzODh5N{Ww
human TF1 cells M13lPWZ2dmO2aX;uJIF{e2G7 M2PHOlIxKG2rboO= NID0NGtKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkCgcYlveyCob3zsc5dm\CCkeTDJUFYh[2ijbHzlcodmKG[xcjCzNEBucW6|IHnuJJBz\XOnbnPlJI9nKHeqb3zlJIJtd2:m78{MJGVEPTB;NEOgcm0v NX[2UXVIOjN4NUmyNVQ>
mouse CTLL cells MV;GeY5kfGmxbjDhd5NigQ>? MoTNTY5pcWKrdHnvckBw\iCMYXuzMY1m\GmjdHXkJGlNOi2rbnT1Z4VlKFO2YYS1JJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDDWGxNKGOnbHzzJIJ6KGOnbHytZoF{\WRiYYPzZZktKEmFNUC9OFghdk1w Mlu2NlEyPTV4MEW=
Ba/F3 cells NUX3Z|JHTnWwY4Tpc44h[XO|YYm= M2HjWFYxKG2rboO= NEHTRWdKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDKRWs{KGW6cILld5Nm\CCrbjDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCjZoTldkA3OCCvaX7zJIJ6KEGucHjhV4Nz\WWwIHHzd4F6NCCLQ{WwQVU1KG6PLh?= MWqyNlA5Pzd3MB?=
monkey T cells MVTGeY5kfGmxbjDhd5NigQ>? NHXCb4pKdmirYnn0bY9vKG:oIHHscI9o\W6rYzDj[Yxtey2|dHnteYxifGWmIIDyc4xq\mW{YYTpc44hcW5ibX;ub4V6KFRiY3XscJMh[nlibXn4[YQhdHmvcHjvZ5l1\SC{ZXHjeIlwdiCvZYToc4QtKEmFNUC9OVchdk1w NVHqfGg2OTR3OUOxPFI>
human monocytes MV3GeY5kfGmxbjDhd5NigQ>? MUTJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44tKEmFNUC9NE4yQDRizszNMi=> NH;XZoIzOzV2ME[0PC=>
human HUO3 cells MoXLSpVv[3Srb36gZZN{[Xl? MU[0JIRigXN? M1SwRmlvcGmkaYTpc44hd2ZiaIXtZY4hT01vQ2PGMYlv\HWlZXSgdJJwdGmoZYLheIlwdiCrbjDoeY1idiCKVV:zJINmdGy|IHHzd4V{e2WmIHHzJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NF0xNjN{NDFOwG0v Moi5NVQ2QTNzOEK=
mouse BAF3 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 MnrLO|IhcA>? NHTNXIxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOg[ZhxemW|c3nu[{BVTUxvSlHLN{BscW6jc3WgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTBwNUeg{txONg>? NITHUIUyQTd4MkKzPC=>
human NK92 cells M1LEdmZ2dmO2aX;uJIF{e2G7 NUPNc25VOjBibXnudy=> M4WzU2lvcGmkaYTpc44hd2ZiVGnLNkBqdiCqdX3hckBPUzl{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxzMj3pcoR2[2WmIGPURXQ1KHCqb4PwbI9zgWyjdHnvckBqdmO3YnH0[YQh\m:{IEKwJI1qdnNiZn;scI94\WRiYomgTWwyOiClaHHscIVv\2ViZn;yJFQ2KG2rboOsJGVEPTB;MD63NUDPxE1w MUeyN|Y2QTJzNB?=
TF1 cells NFnWTWNHfW6ldHnvckBie3OjeR?= NHnEOXZKdmirYnn0bY9vKG:oIFnMN{1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gWGYyKGOnbHzz89yNKEmFNUC9NE45KM7:TT6= MXqxOlk{PDR3Nx?=
human Jurkat cells M3nLVGZ2dmO2aX;uJIF{e2G7 MWCyOEBp NGnQbnhKdmirYnn0bY9vKG:oIHHueIkuS0R|L3HueIkuS0R{OD3pcoR2[2WmIFnMNkBxem:mdXP0bY9vKGmwIHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiB{NDDodpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3ME23Mlg1KM7:TT6= NFLmfYIyPDV7M{G4Ni=>
human TALL-1 cells NH7NbXZHfW6ldHnvckBie3OjeR?= NITIcYxKdmirYnn0bY9vKG:oIFrBT|MhcW5iaIXtZY4hXEGOTD2xJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVytNkBqdmS3Y3XkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCjdDCxJJVOKHC{ZXnuZ5Vj[XSnZDDmc5IhOyCqcoOg[o9tdG:5ZXSgZpkhUUxvMjDpcoR2[3Srb36gcYVie3W{ZXSgZYZ1\XJiM{CgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? NH72VHgzPjJ3OEWyNS=>
human DND/L12 cells Mk\HSpVv[3Srb36gZZN{[Xl? NFPhT3M{OCCvaX7z Mo\HTY5pcWKrdHnvckBw\iCMQVuzJIlvKGi3bXHuJGRPTC:OMUKgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCudXPp[oVz[XOnIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJIh2dWGwIIPldpVuKGGuYoXtbY4v MVmxOFU6OzF6Mh?=
human YT cells MYjGeY5kfGmxbjDhd5NigQ>? MYKzNEBv\y:vbB?= M1P6OmlvcGmkaYTpc44hd2ZiSVyyMYlv\HWlZXSgTmFMOyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hYVRiY3XscJMh[XRiM{CgcocwdWxiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NI\OO2YyPDV7M{G4Ni=>
human OCL-AML5 cells MXPGeY5kfGmxbjDhd5NigQ>? NH64TXQyKM7:TR?= M2D5cVMhcA>? NUPJW2hMUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKE:FTD3BUWw2KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OIIHnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJIF1KDFidV2gdJJmcW6ldXLheIVlKG[xcjCzJIhzeyCob3zsc5dm\CCkeTDHUU1EW0ZiaX7keYN1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliaX3teY5w[myxdITpcoc> MWmyOlI2QDV{MR?=
human CD4+ T cells MWjGeY5kfGmxbjDhd5NigQ>? NVO1SXdFPSC2bzC1NFAhdk1? M4ToNlEhcA>? M4XZOGlvcGmkaYTpc44hd2ZiSVyyMYlv\HWlZXSgV5RifDVicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEOGNDugWEBk\WyuczDheEA2KHSxIEWwNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfA>? MWWxPVA2Ozd3Nh?=
human Huh7 cells NYnaO|NJTnWwY4Tpc44h[XO|YYm= NXi2UVFEOTBizszN MWmzNEBucW6| M{XKV2lvcGmkaYTpc44hd2ZiVInrNkBqdiCqdX3hckBJfWh5IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBKTk6jbIDoZVUucW6mdXPl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYYSgNVAhfU1icILlMYlv[3WkYYTl[EBnd3JiM{CgcYlveyCkZX\vdoUhUU[QYXzwbIE2KHO2aX31cIF1cW:wIH\vdkA{OCCvaX7zJI1qdnNiYomgbY1ufW6xYnzveJRqdmd? NELhXpYzPjJ|MUG1PS=>
human Hs578T cells NFzCeHlHfW6ldHnvckBie3OjeR?= MXmzJO69VQ>? MWixOkBp M{Hadmlv\HWldHnvckBw\iCSVGDOOkBqdiCqdX3hckBJezV5OGSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOyC3TTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBx\XK4YX7h[IF1\Q>? M{DIelI1QTd6MUGy
human SUM149PT cells MXfGeY5kfGmxbjDhd5NigQ>? NHrHdFE{KM7:TR?= Mn;LNVYhcA>? MYPJcoR2[3Srb36gc4YhWFSSTk[gbY4hcHWvYX6gV3VOOTR7UGSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOyC3TTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBx\XK4YX7h[IF1\Q>? NHfNbnYzPDl5OEGxNi=>
human Huh7 cells NF3sRllHfW6ldHnvckBie3OjeR?= M1vNOFExKM7:TR?= M4C5cVMxKG2rboO= MnrhTY5pcWKrdHnvckBw\iCWeXuyJIlvKGi3bXHuJGh2cDdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIJie2GuIHzleoVtKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDh[pRmeiB|MDDtbY5{KGK7IHntcZVvd2Kub4T0bY5o Mn3GNlYzOzFzNUm=
human UT7 cells NUDP[YZ1TnWwY4Tpc44h[XO|YYm= NXfwOI5RUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFWWNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCHUF:td5RqdXWuYYTl[EBUXEGWNTDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= NUDSSZc6OjZ|N{K2OVM>

... Click to View More Cell Line Experimental Data

体内研究 CP-690550 作用于小鼠模型,降低迟发型超敏感反应和延长心脏移植存活。而且, CP-690550 处理来自JAK2V617F阳性 PV患者体内外膨胀的红系祖细胞,产生特定的抗增殖(IC50 = 0.2 µM) 和促凋亡活性。 相反, 在增殖(IC50 > 1.0 µM)和凋亡检测时,从健康对照组中的膨胀祖细胞对CP-690550敏感性低很多。 [2] CP-690550按 10和30 mg/kg剂量每天处理NK细胞,持续处理2周,与对照组相比,细胞数显著降低,这种作用存在时间依赖性。 CP-690550处理实验组的动物效应小样记忆CD8+ 细胞数比对照组低55% 。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

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酶实验:

进行JAK1, JAK2, 和JAK3 激酶实验,使用在杆状病毒感染的 SF9细胞中表达的蛋白(GST 和人类JAK酶催化结构域的融合蛋白),通过亲和层析在谷胱甘肽-琼脂糖凝胶中纯化。反应底物是聚谷氨酸-酪氨酸 [PGT (4:1)], 按100 μg/mL包被到Nunc Maxi Sorp板上,在 37oC下过夜。然后冲洗板三次, 在每孔中加入JAK 酶,孔中含100 μL激酶buffer(50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM 钒酸钠)。按不同剂量加入CP-690550,进行激酶实验。然后在室温下温育30分钟,再冲洗实验板三次。通过标准ELISA实验,使用 磷酸化抗体测定一个给定孔中的磷酸化的酪氨酸水平。
细胞实验:

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  • Cell lines: HEL细胞, 扩增的红系祖细胞
  • Concentrations: 0.1 μM,1 μM
  • Incubation Time: 40分钟
  • Method:

    HEL细胞, 从正常供着,两个PV病人体内获得的扩大红系祖细胞,和 FDCP-EpoR受体细胞(每组样本2 × 107 个细胞),使用浓度不断增高的 CP-690550处理, 然后在不同时间点收集。细胞制成颗粒,使用冷磷酸盐缓冲液冲洗三次,然后悬浮在300 µL裂解液中 ,再在冰上处理1小时。细胞裂解液按20 000g转速在 4oC下离心20分钟,取出上清液。在上清液中加入15 µL anti-JAK2 (处理细胞) 或 anti-JAK3 兔抗体(未处理细胞),然后在冰上再处理1小时。最后, 在上清液中加入50 µL 蛋白A/G琼脂糖浆,然后在 4oC下不断旋转温育过夜。冲洗抗体-蛋白复合体三次, 再使用放射免疫沉淀法(RIPA) buffer冲洗一次,使用冲洗冲洗一次,最后使用50 mM Tris-HCl buffer pH 为7.5冲洗一次。通过 Western blotting 分析免疫沉淀复合物,使用磷酸酪氨酸抗体,除去,再使用anti-JAK2和anti-JAK3抗体做探针,来分析免疫沉淀复合物。


    (Only for Reference)
动物实验:

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  • Animal Models: 毛里求斯成年猕猴
  • Formulation: 在溶于蒸馏水的0.5%甲基纤维素中配制
  • Dosages: 10, 30 mg/kg/d
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (198.21 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% methylcellulose
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 504.49
化学式

C16H20N6O.C6H8O7

CAS号 540737-29-9
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

JAK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID