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 45 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 NFzvfpFHfW6ldHnvckBie3OjeR?= MkP2N|AhdWmwcx?= M3vvRWlvcGmkaYTpc44hd2ZiaIXtZY4hT1OWLX\1d4VlKEqDS{OgZ4F1[Wy7dHnjJIRwdWGrbjDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiU3[5JINmdGy|IIXzbY5oKHCxbInncJV1[W2rYzDhZ4llNXS7cn;zbY5mKGG|IIP1ZpN1emG2ZTDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCNaU2wMlQhdk1w NED2[WYzOzZ4OES4OC=>
Sf9 cells NGSwNVZHfW6ldHnvckBie3OjeR?= M3zZd|kxKG2rboO= MYPJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KE5vdHXycYlv[WxiR2PUMZRi\2enZDDKRWs{KGW6cILld5Nm\CCrbjDT[lkh[2WubIOgeZNqdmdiQnnveIlvNUyFLVXRSWRGWEWJRGnGSXdNTSCjczDzeYJ{fHKjdHWgZYZ1\XJiOUCgcYlveyCkeTDUVk1HWkWWIHHzd4F6NCCLQ{WwQVAvPiCwTT6= MUGyNlA5Pzd3MB?=
SF21 cells NY\jPYc4TnWwY4Tpc44h[XO|YYm= NGTRPXUyOCCvaX7z MnHlTY5pcWKrdHnvckBw\iCMQVuyJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKFOIMkGgZ4VtdHNidYPpcochSmmxdHnuMWtCUUWWRFvFXXlVXkuGIHHzJJN2[nO2cnH0[UBidmRiW{OzVIdidW2jXVHUVEBqdmO3YnH0[YQh\m:{IEGwJI1qdnNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliVH;wZ492dnRiYX7hcJl{cXNuIFnDOVA:PCCwTT6= M4WwOVI{PTRzNkew
human MO7 cells MXrGeY5kfGmxbjDhd5NigQ>? M33MS2lvcGmkaYTpc44hd2ZiSnHrN{1u\WSrYYTl[EBKVDF3LXnu[JVk\WRiU4TheFUheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1QPyClZXzsd{BjgSClZXzsMYJie2WmIHHzd4F6NCCLQ{WwQVI1KG6PLh?= MV:yNVE2PTZyNR?=
Ba/F3 cells M1XpdWZ2dmO2aX;uJIF{e2G7 NGr1cG43OCCvaX7z Mmi1TY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiSlHLNUBmgHC{ZYPz[YQhcW5iQnGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDTWGFVPSCyaH;zdIhwenmuYYTpc44h[W[2ZYKgOlAhdWmwczDifUBCdHCqYWPjdoVmdiCjc4PhfUwhUUN3ME2yOkBvVS5? MVuyNlA5Pzd3MB?=
human T cells MmrqSpVv[3Srb36gZZN{[Xl? NILycYVKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvcw+9lCCLQ{WwQVI5KG6PLh?= NGf2eXczOzV2ME[0PC=>
human PBMC MWPGeY5kfGmxbjDhd5NigQ>? M2LSblMxKG2rboO= MkmyTY5pcWKrdHnvckBw\iCMQVuxM2pCUzNiaX6gbJVu[W5iUFLNR{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXR{KHCqb4PwbI9zgWyjdHnvckBxemWrbnP1ZoF1\WRiZn;yJFMxKG2rboOgdJJqd3JidH:gTWwzKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KGmwdILhZ4VtdHWuYYKgdIhwe2[ub4egd5RicW6rbnesJGlEPTB;M{Ogcm0v MYeyNlA5Pzd3MB?=
human TF1 cells M1;iT2Z2dmO2aX;uJIF{e2G7 NISzeZQzOCCvaX7z MX7Jcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWw3NWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHnuZ5Vj[XSnZDDmc5IhOjBibXnud{Bnd2yub4fl[EBjgSCLTE[gZ4hidGynbnflJIZweiB|MDDtbY5{KGmwIIDy[ZNmdmOnIH;mJJdpd2ynIHLsc49l97zOIFXDOVA:PDNibl2u M4nY[VI{PjV7MkG0
mouse CTLL cells MonzSpVv[3Srb36gZZN{[Xl? NWO2dY9uUW6qaXLpeIlwdiCxZjDKZYs{NW2nZHnheIVlKEmOMj3pcoR2[2WmIGP0ZZQ2KHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBEXEyOIHPlcIx{KGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVA:PDhibl2u MlvGNlEyPTV4MEW=
Ba/F3 cells MlzoSpVv[3Srb36gZZN{[Xl? NUHSdmZQPjBibXnudy=> M2P0bWlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIFrBT|Mh\XiycnXzd4VlKGmwIFLhM2Y{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGGodHXyJFYxKG2rboOgZpkhSWyyaHHTZ5Jm\W5iYYPzZZktKEmFNUC9OVQhdk1w NWDydGlXOjJyOEe3OVA>
monkey T cells MoHrSpVv[3Srb36gZZN{[Xl? M4nCe2lvcGmkaYTpc44hd2ZiYXzsc4dmdmmlIHPlcIx{NXO2aX31cIF1\WRicILvcIln\XKjdHnvckBqdiCvb37r[ZkhXCClZXzsd{BjgSCvaYjl[EBtgW2yaH;jfZRmKHKnYXP0bY9vKG2ndHjv[EwhUUN3ME21O{BvVS5? NXrxTWVJOTR3OUOxPFI>
human monocytes MXPGeY5kfGmxbjDhd5NigQ>? MWrJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44tKEmFNUC9NE4yQDRizszNMi=> NX;qOVBXOjN3NEC2OFg>
human HUO3 cells NWXl[YFPTnWwY4Tpc44h[XO|YYm= MmnLOEBl[Xm| NV\2[YpEUW6qaXLpeIlwdiCxZjDoeY1idiCJTT3DV2YucW6mdXPl[EBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjVU|Mh[2WubIOgZZN{\XO|ZXSgZZMhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGGodHXyJFQh\GG7czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwM{K0JO69VS5? MWSxOFU6OzF6Mh?=
mouse BAF3 cells Ml;hVJJwdGmoZYLheIlwdiCjc4PhfS=> NX3zWm5MPzJiaB?= NE[3NI9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOg[ZhxemW|c3nu[{BVTUxvSlHLN{BscW6jc3WgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTBwNUeg{txONg>? MYCxPVc3OjJ|OB?=
human NK92 cells MV\GeY5kfGmxbjDhd5NigQ>? MmHiNlAhdWmwcx?= MU\Jcohq[mm2aX;uJI9nKFS\S{KgbY4hcHWvYX6gUms6OiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOTJvaX7keYNm\CCVVFHUOEBxcG:|cHjvdplt[XSrb36gbY5kfWKjdHXkJIZweiB{MDDtbY5{KG[xbHzve4VlKGK7IFnMNVIh[2ijbHzlcodmKG[xcjC0OUBucW6|LDDFR|UxRTBwN{Gg{txONg>? MXuyN|Y2QTJzNB?=
TF1 cells Ml\wSpVv[3Srb36gZZN{[Xl? M2jqXWlvcGmkaYTpc44hd2ZiSVyzMYlv\HWlZXSgdJJwdGmoZYLheIlwdiCxZjDUSlEh[2WubIRvwKwhUUN3ME2wMlgh|ryPLh?= NHjD[mYyPjl|NES1Oy=>
human Jurkat cells MVjGeY5kfGmxbjDhd5NigQ>? NEP0bWczPCCq NV;GWWlkUW6qaXLpeIlwdiCxZjDhcpRqNUOGMz;hcpRqNUOGMkitbY5lfWOnZDDJUFIheHKxZIXjeIlwdiCrbjDoeY1idiCMdYLrZZQh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUC9O{45PCEQvF2u Ml\lNVQ2QTNzOEK=
human TALL-1 cells NUCzU4NRTnWwY4Tpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKEqDS{OgbY4hcHWvYX6gWGFNVC1zIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUxvMjDpcoR2[2WmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBifCBzIIXNJJBz\WmwY4XiZZRm\CCob4KgN{BpenNiZn;scI94\WRiYomgTWwuOiCrbnT1Z5Rqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCrbX31co9jdG:2dHnu[y=> M3ezTlI3OjV6NUKx
human DND/L12 cells NYPIc2VXTnWwY4Tpc44h[XO|YYm= Ml\mN|AhdWmwcx?= Mn\mTY5pcWKrdHnvckBw\iCMQVuzJIlvKGi3bXHuJGRPTC:OMUKgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCudXPp[oVz[XOnIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJIh2dWGwIIPldpVuKGGuYoXtbY4v NFnKTFYyPDV7M{G4Ni=>
human YT cells M{fS[2Z2dmO2aX;uJIF{e2G7 MnywN|AhdmdxbXy= M4e1U2lvcGmkaYTpc44hd2ZiSVyyMYlv\HWlZXSgTmFMOyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hYVRiY3XscJMh[XRiM{CgcocwdWxiYomgbY1ufW6xYnzveJRqdmdiYX7hcJl{cXN? NEHtc20yPDV7M{G4Ni=>
human OCL-AML5 cells MmPSSpVv[3Srb36gZZN{[Xl? M2\URlEh|ryP NYW1T445OyCq Mk[zTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJG9EVC2DTVy1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiR12tR3NHKGmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIHH0JFEhfU1icILlbY5kfWKjdHXkJIZweiB|IHjyd{Bnd2yub4fl[EBjgSCJTT3DV2YhcW6mdXP0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhcW2vdX7vZoxwfHSrbne= MlrsNlYzPTh3MkG=
human CD4+ T cells NFPifXZHfW6ldHnvckBie3OjeR?= M3nNdlUhfG9iNUCwJI5O MlPONUBp NHruPVRKdmirYnn0bY9vKG:oIFnMNk1qdmS3Y3XkJHN1[XR3IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCFRESrJHQh[2WubIOgZZQhPSC2bzC1NFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3R? MkDPNVkxPTN5NU[=
human Huh7 cells NHO0e45HfW6ldHnvckBie3OjeR?= NWHMZppYOTBizszN NE\lXGo{OCCvaX7z MXzJcohq[mm2aX;uJI9nKFS7a{KgbY4hcHWvYX6gTJVpPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTWZP[WyyaHG1MYlv\HWlZXSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKGG2IEGwJJVOKHC{ZT3pcoN2[mG2ZXSg[o9zKDNyIH3pcpMh[mWob4LlJGlHVmGucHjhOUB{fGmvdXzheIlwdiCob4KgN|AhdWmwczDtbY5{KGK7IHntcZVvd2Kub4T0bY5o NHzLN3gzPjJ|MUG1PS=>
human Hs578T cells MX3GeY5kfGmxbjDhd5NigQ>? NGrCcXI{KM7:TR?= NFW5PZkyPiCq NIXEZ5ZKdmS3Y4Tpc44hd2ZiUGTQUlYhcW5iaIXtZY4hUHN3N{jUJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KDNidV2gZYZ1\XJiMU[gbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXNiaX6gdJJme2WwY3Wgc4YheGW{dnHuZYRifGV? NVuxWolqOjR7N{ixNVI>
human SUM149PT cells NILPZoZHfW6ldHnvckBie3OjeR?= NFX4O4I{KM7:TR?= M3TtRlE3KGh? MXHJcoR2[3Srb36gc4YhWFSSTk[gbY4hcHWvYX6gV3VOOTR7UGSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhOyC3TTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBx\XK4YX7h[IF1\Q>? M1HZSVI1QTd6MUGy
human Huh7 cells NEL5RpRHfW6ldHnvckBie3OjeR?= NF3XTlQyOCEQvF2= MXOzNEBucW6| NHzLcZFKdmirYnn0bY9vKG:oIGT5b|IhcW5iaIXtZY4hUHWqNzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[mG|YXygcIV3\WxiU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KDFyIIXNJIFnfGW{IEOwJI1qdnNiYomgbY1ufW6xYnzveJRqdmd? M334e|I3OjNzMUW5
human UT7 cells Mkf1SpVv[3Srb36gZZN{[Xl? NVjuS5Z3UW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFWWNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCHUF:td5RqdXWuYYTl[EBUXEGWNTDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= NWnCd|ZLOjZ|N{K2OVM>

... 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]

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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

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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 --

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