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 43 Publications

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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 NELmUmpHfW6ldHnvckBie3OjeR?= MlHON|AhdWmwcx?= NV[wZllZUW6qaXLpeIlwdiCxZjDoeY1idiCJU2St[pV{\WRiSlHLN{Bk[XSjbIn0bYMh\G:vYXnuJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3cz3pcoZm[3SnZDDT[lkh[2WubIOgeZNqdmdicH;sfYdtfXSjbXnjJIFkcWRvdInyc5NqdmViYYOgd5Vje3S{YYTlJIFnfGW{IEOwJI1qdnNiYomgSWxKW0FuIFvpQVAvPCCwTT6= M3flVlI{PjZ6NEi0
Sf9 cells NHvzVYhHfW6ldHnvckBie3OjeR?= MnHIPVAhdWmwcx?= M1HKOWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiTj30[ZJucW6jbDDHV3QufGGpZ3XkJGpCUzNiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{B2e2mwZzDCbY91cW5vTFOtSXFGTEWSRVfEXWZGX0yHIHHzJJN2[nO2cnH0[UBi\nSncjC5NEBucW6|IHL5JHRTNU[URWSgZZN{[XluIFnDOVA:OC54IH7NMi=> M4i2flIzODh5N{Ww
SF21 cells MUjGeY5kfGmxbjDhd5NigQ>? MWSxNEBucW6| NUjXNWY3UW6qaXLpeIlwdiCxZjDKRWszKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGPGNlEh[2WubIOgeZNqdmdiQnnveIlvNUuDSVXUSGtGYVmWVlvEJIF{KHO3YoP0doF1\SCjbnSgX|M{WGejbX3hYWFVWCCrbnP1ZoF1\WRiZn;yJFExKG2rboOgdJJqd3JidH:gd5Vje3S{YYTlJIFl\Gm2aX;uJI1m[XO3cnXkJIFnfGW{IEOwJI1qdnNiYomgWI9x[2:3boSgZY5idHm|aYOsJGlEPTB;NDDuUU4> M3\2bVI{PTRzNkew
human MO7 cells M2DteWZ2dmO2aX;uJIF{e2G7 M1ywfWlvcGmkaYTpc44hd2ZiSnHrN{1u\WSrYYTl[EBKVDF3LXnu[JVk\WRiU4TheFUheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1QPyClZXzsd{BjgSClZXzsMYJie2WmIHHzd4F6NCCLQ{WwQVI1KG6PLh?= NIr4WYYzOTF3NU[wOS=>
Ba/F3 cells MVfGeY5kfGmxbjDhd5NigQ>? NELTWXc3OCCvaX7z MmO1TY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiSlHLNUBmgHC{ZYPz[YQhcW5iQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgOlAhdWmwczDifUBCdHCqYWPjdoVmdiCjc4PhfUwhUUN3ME2yOkBvVS5? MWiyNlA5Pzd3MB?=
human T cells MX\GeY5kfGmxbjDhd5NigQ>? NEPQ[JBKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvcw+9lCCLQ{WwQVI5KG6PLh?= NFHUdmMzOzV2ME[0PC=>
human PBMC NX\pWIV[TnWwY4Tpc44h[XO|YYm= M4X5PFMxKG2rboO= MonmTY5pcWKrdHnvckBw\iCMQVuxM2pCUzNiaX6gbJVu[W5iUFLNR{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXR{KHCqb4PwbI9zgWyjdHnvckBxemWrbnP1ZoF1\WRiZn;yJFMxKG2rboOgdJJqd3JidH:gTWwzKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KGmwdILhZ4VtdHWuYYKgdIhwe2[ub4egd5RicW6rbnesJGlEPTB;M{Ogcm0v MkTTNlIxQDd5NUC=
human TF1 cells NF7TVo1HfW6ldHnvckBie3OjeR?= M2mwNVIxKG2rboO= MoTXTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDpcoN2[mG2ZXSg[o9zKDJyIH3pcpMh\m:ubH;3[YQh[nliSVy2JINp[WyuZX7n[UBnd3JiM{CgcYlveyCrbjDwdoV{\W6lZTDv[kB4cG:uZTDicI9w\O,:jDDFR|UxRTR|IH7NMi=> MX2yN|Y2QTJzNB?=
mouse CTLL cells NWjVdWV1TnWwY4Tpc44h[XO|YYm= NX2wPHdRUW6qaXLpeIlwdiCxZjDKZYs{NW2nZHnheIVlKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBEXEyOIHPlcIx{KGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVA:PDhibl2u NXjMbZFSOjFzNUW2NFU>
Ba/F3 cells MmfwSpVv[3Srb36gZZN{[Xl? M4q4VlYxKG2rboO= MY\Jcohq[mm2aX;uJI9nKFSHTD3meZNm\CCMQVuzJIV5eHKnc4Pl[EBqdiCEYT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBi\nSncjC2NEBucW6|IHL5JGFteGijU3Py[YVvKGG|c3H5MEBKSzVyPUW0JI5ONg>? MkDINlIxQDd5NUC=
monkey T cells NEfQTZNHfW6ldHnvckBie3OjeR?= Mk[3TY5pcWKrdHnvckBw\iCjbHzv[4VvcWNiY3XscJMue3SrbYXsZZRm\CCycn;sbYZmemG2aX;uJIlvKG2xbnvlfUBVKGOnbHzzJIJ6KG2reHXkJIx6dXCqb3P5eIUhemWjY4Tpc44hdWW2aH;kMEBKSzVyPUW3JI5ONg>? MYGxOFU6OzF6Mh?=
human monocytes NEm4O5JHfW6ldHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44tKEmFNUC9NE4yQDRizszNMi=> MV2yN|U1ODZ2OB?=
human HUO3 cells NVjNS2VOTnWwY4Tpc44h[XO|YYm= M2nWe|Qh\GG7cx?= M3rJbGlvcGmkaYTpc44hd2ZiaIXtZY4hT01vQ2PGMYlv\HWlZXSgdJJwdGmoZYLheIlwdiCrbjDoeY1idiCKVV:zJINmdGy|IHHzd4V{e2WmIHHzJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NF0xNjN{NDFOwG0v NVW4UVk{OTR3OUOxPFI>
mouse BAF3 cells M{PtT3Bzd2yrZnXyZZRqd25iYYPzZZk> NUnF[2VIPzJiaB?= NFzRS5RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOg[ZhxemW|c3nu[{BVTUxvSlHLN{BscW6jc3WgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTBwNUeg{txONg>? MVOxPVc3OjJ|OB?=
human NK92 cells M2P5TWZ2dmO2aX;uJIF{e2G7 M134SlIxKG2rboO= MorPTY5pcWKrdHnvckBw\iCWWVuyJIlvKGi3bXHuJG5MQTJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDF{LXnu[JVk\WRiU2TBWFQheGixc4Doc5J6dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkCgcYlveyCob3zsc5dm\CCkeTDJUFEzKGOqYXzs[Y5o\SCob4KgOFUhdWmwczygSWM2OD1yLkexJO69VS5? MkCzNlM3PTl{MUS=
TF1 cells NEPiZ49HfW6ldHnvckBie3OjeR?= MnP5TY5pcWKrdHnvckBw\iCLTEOtbY5lfWOnZDDwdo9tcW[ncnH0bY9vKG:oIGTGNUBk\Wyuc,-8kEBKSzVyPUCuPEDPxE1w NYD5WY1iOTZ7M{S0OVc>
human Jurkat cells NFnyR4xHfW6ldHnvckBie3OjeR?= M1XFVVI1KGh? NIfxSldKdmirYnn0bY9vKG:oIHHueIkuS0R|L3HueIkuS0R{OD3pcoR2[2WmIFnMNkBxem:mdXP0bY9vKGmwIHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiB{NDDodpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3ME23Mlg1KM7:TT6= NYHxRmh6OTR3OUOxPFI>
human TALL-1 cells NGLObWRHfW6ldHnvckBie3OjeR?= Mlv0TY5pcWKrdHnvckBw\iCMQVuzJIlvKGi3bXHuJHRCVExvMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmOLUKgbY5lfWOnZDDTWGFVPSCyaH;zdIhwenmuYYTpc44h[XRiMTD1UUBxemWrbnP1ZoF1\WRiZn;yJFMhcHK|IH\vcIxwf2WmIHL5JGlNNTJiaX7keYN1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliaX3teY5w[myxdITpcoc> MWiyOlI2QDV{MR?=
human DND/L12 cells M2n2UWZ2dmO2aX;uJIF{e2G7 Mm\6N|AhdWmwcx?= MVXJcohq[mm2aX;uJI9nKEqDS{OgbY4hcHWvYX6gSG5FN0xzMjDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KGy3Y3nm[ZJie2ViYYPzZZkhcW5icILld4Vv[2Vib3[gbJVu[W5ic3XyeY0h[WykdX3pck4> MnLtNVQ2QTNzOEK=
human YT cells M4jKZ2Z2dmO2aX;uJIF{e2G7 MnvnN|AhdmdxbXy= NHLvN3VKdmirYnn0bY9vKG:oIFnMNk1qdmS3Y3XkJGpCUzNicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFmWIHPlcIx{KGG2IEOwJI5oN22uIHL5JIludXWwb3Lsc5R1cW6pIHHuZYx6e2m| M4fFZ|E1PTl|MUiy
human OCL-AML5 cells NGrRPGdHfW6ldHnvckBie3OjeR?= NWe0[FBmOSEQvF2= NX2w[YY6OyCq Mn\vTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJG9EVC2DTVy1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiR12tR3NHKGmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIHH0JFEhfU1icILlbY5kfWKjdHXkJIZweiB|IHjyd{Bnd2yub4fl[EBjgSCJTT3DV2YhcW6mdXP0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhcW2vdX7vZoxwfHSrbne= Mn[0NlYzPTh3MkG=
human CD4+ T cells NHHq[WJHfW6ldHnvckBie3OjeR?= MoqwOUB1dyB3MECgcm0> NITJSpUyKGh? MWPJcohq[mm2aX;uJI9nKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBETDRtIGSgZ4VtdHNiYYSgOUB1dyB3MECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Q> NWW5NWNPOTlyNUO3OVY>
human Huh7 cells NX;Zc2o1TnWwY4Tpc44h[XO|YYm= M2XHVVExKM7:TR?= M4fXcFMxKG2rboO= MoHETY5pcWKrdHnvckBw\iCWeXuyJIlvKGi3bXHuJGh2cDdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGlHVmGucHjhOU1qdmS3Y3XkJHNVSVR|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCycnWtbY5kfWKjdHXkJIZweiB|MDDtbY5{KGKnZn;y[UBKTk6jbIDoZVUhe3SrbYXsZZRqd25iZn;yJFMxKG2rboOgcYlveyCkeTDpcY12dm:kbH;0eIlv\w>? NEHn[ogzPjJ|MUG1PS=>
human Hs578T cells NFTkc2VHfW6ldHnvckBie3OjeR?= NXX2eZJWOyEQvF2= MXGxOkBp Mke3TY5lfWO2aX;uJI9nKFCWUF62JIlvKGi3bXHuJGh{PTd6VDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEA{KHWPIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJJBmen[jbnHkZZRm NVLIdnhEOjR7N{ixNVI>
human SUM149PT cells MWDGeY5kfGmxbjDhd5NigQ>? MYCzJO69VQ>? NIrDVHEyPiCq NVPvbm01UW6mdXP0bY9vKG:oIGDUVG43KGmwIHj1cYFvKFOXTUG0PXBVKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9vKGG2IEOgeW0h[W[2ZYKgNVYhcHK|IHL5JHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYOgbY4heHKnc3XuZ4Uhd2ZicHXyeoFv[WSjdHW= MV2yOFk4QDFzMh?=
human Huh7 cells NFfnR|JHfW6ldHnvckBie3OjeR?= M3HSU|ExKM7:TR?= M2S3RlMxKG2rboO= MV\Jcohq[mm2aX;uJI9nKFS7a{KgbY4hcHWvYX6gTJVpPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gZoF{[WxibHX2[YwhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JFExKHWPIHHmeIVzKDNyIH3pcpMh[nliaX3teY5w[myxdITpcoc> MoXRNlYzOzFzNUm=
human UT7 cells NUD3[|gxTnWwY4Tpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWXQ4KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGVRVy2|dHnteYxifGWmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBjgSCDbIDoZXNkemWnbjDhd5NigQ>? MUWyOlM4OjZ3Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
JAK3 / STAT5 / p-STAT5; 

PubMed: 27732937     


The following cell lines: EBV-negative B cell line (BJAB), EBV-transformed lymphoblastoid cell line (LCL), EBV-negative T cell lines (Jurkat and MOLT4), EBV-positive T cell lines (SNT15 and SNT16), EBV-negative NK cell line (KHYG1), and EBV-positive NK cell lines (KAI3 and SNK6), were treated without (−) or with (+) 1 μM tofacitinib for 24 h and cell lysates were then immunoblotted for the indicated proteins.

LMP1 / EBNA1 / BZLF1; 

PubMed: 27732937     


SNT13, SNT15, SNT16, KAI3 and SNK6 cell lines were treated with 5 μM tofacitinib for 48 h, and cell lysates were immunoblotted for LMP1, EBNA1 and BZLF1. Actin was blotted as a loading control.

JAK3 / p-JAK3 / STAT3; 

PubMed: 26082451     


CTCL cell lines were subjected to western blot (tofacitinib 10, 100, 200 nM) (G) after 48 hours of treatment.

27732937 26082451
Growth inhibition assay
Cell number; 

PubMed: 27732937     


BJAB, LCL, Jurkat, SNT15, KHYG1 and KAI3 cells were treated with the indicated concentrations of tofacitinib, and viable cells were counted at the indicated times using the trypan blue exclusion test. Values are means ± SE of the results from triplicate experiments. *P < 0.05 as compared with DMSO-treated cells.

27732937
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]

+ Expand
  • 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]

+ Expand
  • 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

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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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04111614 Not yet recruiting Drug: Tofacitinib tablet|Drug: Tofacitinib Oral Solution Healthy Pfizer October 9 2019 Phase 1
NCT03681275 Recruiting Drug: Tofacitinib 5 mg|Drug: Placebo to match Tofacitinib Diaphragm Injury Stanford University September 3 2019 Phase 1
NCT04047121 Active not recruiting -- Rheumatoid Arthritis Pfizer May 20 2019 --
NCT03981900 Recruiting Drug: Tofacitinib Arthritis Rheumatoid Pfizer January 4 2019 --
NCT03800979 Recruiting Drug: Tofacitinib Alopecia Areata Institute of Dermatology Thailand January 12 2019 Phase 4
NCT03964649 Completed -- Arthritis Rheumatoid Pfizer January 1 2019 --

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

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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