Ruxolitinib (INCB018424)

Catalog No.S1378

Ruxolitinib (INCB018424) Chemical Structure

Molecular Weight(MW): 306.37

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

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Cited by 36 Publications

5 Customer Reviews

  • STAT3 phosphorylation as determined by phospho flow, mixed lymphocyte reactions containing BALB/c spleen-derived CD4+ T cells co-cultured with or without C57BL/6 BM-derived DC preactivated with 20 ng/mL LPS.

    Blood 2014 123(24), 3832-42. Ruxolitinib (INCB018424) purchased from Selleck.

    BMDMs were isolated from wild-type mice and incubated in the different concentrations of Ruxolitinib for 1 h before stimulation with 500 U/ml IFN-β for 30 min. Levels of GAPDH as well as total and phospho-Tyr705 STAT3 were determined by immunoblotting.

    J Immunol 2012 189(6), 2784-92. Ruxolitinib (INCB018424) purchased from Selleck.

  • Miniscule 10 PFU amount of VA7-EGFP results in productive infection only in CT26LacZ cells whereas the self-limiting infection can be rescued with JAK/STAT inhibitor Ruxolitinib in CT26WT cells counteracting also the effects of exogenous IFNβ (100 U/ml) pre-treatment. Scale bar: 200 um.

    Gene Ther 2014 10.1038/gt.2014.83. Ruxolitinib (INCB018424) purchased from Selleck.

    INCB018424 administration reverses the protective effects of ALA on ONC retinas. A-C: Representative micrographs (200× magnification) of retinal whole mounts obtained from three groups stained with anti-RNA-binding protein with multiple splicing (Rbpms) antibody (green). Sampling location: 2 mm temporal to the optic disc. Sampling field size: 439 × 330 μm2 (20× objective lens). Scale bar: 50 μm. D: Quantitative analysis of Rbpms-positive cells under different experimental conditions (mean ± standard error of the mean [SEM], n = 6 per group). The average number of Rbpms-positive cells/mm2 was calculated. ONC = optic nerve crush animal; ALA-ONC = alpha lipoic acid (ALA) animal pretreated 1 day before ONC; ALA-ONC+I = ALA animal pretreated 1 day before ONC, followed by INCB018424. *** p<0.001, ** p<0.01 compared to the ONC group, ### p<0.001 compared to the ALA-ONC group at the same time point

    Mol Vis, 2016, 22:1122-1136. Ruxolitinib (INCB018424) purchased from Selleck.

  •  

    HS578T cells were treated with indicated amount of inhibitor for 18 hr. The cells were lysed by cell lysis buffer (20 mM Tris-Cl (pH 8.0); 0.5 M NaCl; 0.25% Triton X-100; 1 mM EDTA; 1 mM EGTA; 10 mM β-glycerophosphate; 10 mM NaF; 300 µM Na3VO4; 1 mM benzamidine) containing 1 mM DTT and 2 µM PMSF. Western blot analyses were performed using cleared cell lysates resolved on sodium dodecyl sulfate (SDS)-polyacrylamide gels, transferred onto polyvinylidene difluoride (PVDF) membranes (Millipore, Billerica, MA), and probed with specific antibodies using standard procedures. Chemiluminescence reagent was purchased from  Thermo Scientific (Rockford, IL). Horseradish peroxidase-conjugated secondary antibodies from Sigma (St. Louis, MO).

    Yong Weon Yi Georgetown University. Ruxolitinib (INCB018424) purchased from Selleck.

Purity & Quality Control

Choose Selective JAK Inhibitors

Biological Activity

Description Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.
Targets
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
2.8 nM 3.3 nM
In vitro

INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424 (64 nM) results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. INCB018424 inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 of 407 nM and 223 nM, respectively. INCB018424 demonstrates remarkable potency against erythroid colony formation with IC50 of 67nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TF1 NXfXeFZMU2mwYYPlJGF{e2G7 MlXXNlAhdWmw MWjEUXNQ MVPJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzMt88US=> Mnu3NlI3QThyOES=
TF1 NIT0U|NMcW6jc3WgRZN{[Xl? NF7OSHYzOCCvaX6= NX3pRppFTE2VTx?= NUjld21GUW6qaXLpeIlwdiCxZjDKRWsyKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmONj3pcoR2[2WmIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlTPxE1? MWOyNlY6QDB6NB?=
Human T cell MkDST4lv[XOnIFHzd4F6 MXfJcohq[mm2aX;uJI9nKEqDS{OvNUBqdiCqdX3hckBVKGOnbHzzJIV5eHKnc4PpcochS0R|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVyyMZN1cW23bHH0[YQhW1SDVEXhJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkROwG0> M1[1WVI{PTRyNkS4
Human monocyte NFzSVXFMcW6jc3WgRZN{[Xl? MYLJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI3|ryP M4W4TFI{PTRyNkS4
Human monocyte MYnLbY5ie2ViQYPzZZk> M{nyeGlvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> NXH2WWlOOjN3NEC2OFg>
HEL MYnDfZRwfG:6aXOgRZN{[Xl? MlHzOUDPxE1? NFPoNHc1QCCq MVPDfZRwfG:6aXOgbY5l\Xh;MUKuNkU> MUeyOVk{OTN2OR?=
SET-2 M2izcWN6fG:2b4jpZ{BCe3OjeR?= Mk\BOUDPxE1? MXG0PEBp NFr3T3pEgXSxdH;4bYMhcW6mZYi9NVgvPyV? NFy2XmEzPTl|MUO0PS=>
HT93A MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHK0[Xk{OjBibl2= MUi1JIQ> MkPESG1UVw>? Mke0TY5pcWKrdHnvckBw\iCJQ2OtSkBqdmS3Y3XkJIdz[W63bH;jfZRq[yCmaX\m[ZJmdnSrYYTpc44> M1vHSlI2QDB3OU[y
CMK MmPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rVZmlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVU4OlZibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:w M3;tZlI2OzV{MUK0
CMK MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jJeWlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVY{TCCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTZ|IN88US=> MmfPNlU{PTJzMkS=
CMK Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XMdmlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCZVDDKRWsh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlA4PSEQvF2= MUWyOVM2OjF{NB?=
NCI-H460 M3Pze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXEUXNQ MX3JR|UxRTBwMUOg{txO NHXYNXkzPTJzM{[3NC=>
NCI-H358 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDEUXNQ NXHTOnN6UUN3ME2wMlEh|ryP MYeyOVIyOzZ5MB?=
A549 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjvTm5FVVOR MUfJR|UxRTBwMESg{txO M4\ue|I2OjF|Nkew
A549/DDP MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nMbmROW09? NYDBOohqUUN3ME2wMlIzKM7:TR?= NHPsUpEzPTJzM{[3NC=>
NCI-H1299 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvCUJZJTE2VTx?= NEfVSYVKSzVyPUCuNlgh|ryP M2nkfVI2OjF|Nkew
NCI-H2347 NHH6dYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLzcGpTTE2VTx?= MmP4TWM2OD1yLkG3JO69VQ>? M{PhT|I2OjF|Nkew
A549/DDP MUDGeY5kfGmxbjDBd5NigQ>? NH3VV4g{OCCwTR?= NFrJS4M1QCCq M{\RU2ROW09? NH6y[nJFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w M4rzR|I2OjF|Nkew
NCI-H1299 MXLGeY5kfGmxbjDBd5NigQ>? Mne5N|Ahdk1? NUHjUZVRPDhiaB?= M3jPV2ROW09? NHWzXVRFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w NVPJXmZmOjV{MUO2O|A>
NCI-H2347 NF;YXGVHfW6ldHnvckBCe3OjeR?= MYWzNEBvVQ>? MnS4OFghcA>? MYDEUXNQ NYLlbVN3TGWlcnXhd4UhcW5iQnPsNkBmgHC{ZYPzbY9v NUjpNmVrOjV{MUO2O|A>
A549/DDP MX;BdI9xfG:|aYOgRZN{[Xl? NHLobnU{OCCwTR?= NFW1Tng1QCCq M{nneWROW09? M4PxOWlv\HWldHnvckBw\iCjcH;weI9{cXN? NIrqOZozPTJzM{[3NC=>
NCI-H1299 M3uzVmFxd3C2b4Ppd{BCe3OjeR?= M3v4OlMxKG6P Ml;nOFghcA>? NFH1SGlFVVOR MofZTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NGjNS4wzPTJzM{[3NC=>
NCI-H2347 MYXBdI9xfG:|aYOgRZN{[Xl? MX6zNEBvVQ>? NYrLZXl4PDhiaB?= MlSxSG1UVw>? MnvRTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MYOyOVIyOzZ5MB?=
Hep3B NEm3RWZHfW6ldHnvckBCe3OjeR?= NXvMe5JOOSEQvF2= NIPuWFcyPiCq NXTrO|ZDTE2VTx?= NWDid5VZUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIHHjeIl3\SCVVFHUN{B4cXSqIFnDOVAhd2ZifkWwJO69VQ>? M{TT[VI1PTBzNki5
HepG2 MUfGeY5kfGmxbjDBd5NigQ>? M{HNNlEh|ryP NWOzUop3OTZiaB?= NEWyeY1FVVOR NH\IflNKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9ic3nncoFtKHSxIGPURXQ{ NFLSTowzPDVyMU[4PS=>
Huh7 NVvLN5ByTnWwY4Tpc44hSXO|YYm= NI\5[m4yKM7:TR?= MVOxOkBp NIi3U41FVVOR NF\GR5RKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9ic3nncoFtKHSxIGPURXQ{ NIG5W4ozPDVyMU[4PS=>
BaF3 NW\yO|lbU2mwYYPlJGF{e2G7 MXi4NEBvVQ>? MljyOkBp NHX0XWpFVVOR MU\S[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4bDqFOWQWS1JIlvKEqDS{LWOlE4Ti2vdYTheIVlKEKDRkOtSXBQWiClZXzs M1jw[|I1OjN5N{mx
DLD-1 NWC2S2RCU2mwYYPlJGF{e2G7 MYeyOUDPxE1? M4LUSFQ5KGh? NX6ye2VPTE2VTx?= Mne5TY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= NIf0RXIzPDB3MEW1NC=>
RKO M3:zb2tqdmG|ZTDBd5NigQ>? NYf4R5BYOjVizszN M1PGdlQ5KGh? MoHMSG1UVw>? NEXM[oFKdmirYnn0bY9vKG:oIFrBT|EheGixc4Doc5J6dGG2aX;u MY[yOFA2ODV3MB?=
DLD-1 MXPLbY5ie2ViQYPzZZk> MmjLNlUh|ryP NWT2OFZoPDhiaB?= MljySG1UVw>? MlnjTY5pcWKrdHnvckBw\iCMQVuyJJBpd3OyaH;yfYxifGmxbh?= M2e0UlI1ODVyNUWw
RKO MXHLbY5ie2ViQYPzZZk> MlXrNlUh|ryP MYG0PEBp NVnZZ2ZzTE2VTx?= MX3kc4V{KG6xdDDpcohq[mm2IFrBT|EheGixc4Doc5J6dGG2aX;u NVnOb3N7OjRyNUC1OVA>
DLD-1 NX60OWFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXQVnNmPTBizszN NFTQd|M1QCCq M3P5cmROW09? M3PyVmlEPTB;MUWuOVEh|ryP MWGyOFA2ODV3MB?=
RKO NGXpUWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;scVUxKM7:TR?= MXO0PEBp Mnr4SG1UVw>? NX\0dpVEUUN3ME2xOE44PiEQvF2= M37oTVI1ODVyNUWw
DLD-1 NHrCWYdCeG:ydH;zbZMhSXO|YYm= NIrRNXUzPSEQvF2= M1zZclQ5KGh? M3HPSmROW09? MYfJcoR2[2W|IHHwc5B1d3OrczDifUBi[3SrdnH0bY5oKGOjc4Dhd4UhOw>? M4G1WVI1ODVyNUWw
RKO NFTnOVVCeG:ydH;zbZMhSXO|YYm= NF7Kfo4zPSEQvF2= Mlr3OFghcA>? NWLGfpBDTE2VTx?= NYn3TJNsUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= MmDFNlQxPTB3NUC=
HuH7 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHTOVAh|ryP MYq0PEBp NUHwSotCTE2VTx?= MYO+PFImKHKnZIXjeIlwdg>? M4n0WFI{QTRzOEOy
SNU182 NHv4cWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\kdlUxKM7:TR?= NHnLfpI1QCCq M3rySGROW09? NULJUnFDRjZ2JTDy[YR2[3Srb36= MonWNlM6PDF6M{K=
SNU423 M1TsVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DKRlUxKM7:TR?= MljEOFghcA>? NX;RTVA4TE2VTx?= MonoQlgyLSC{ZXT1Z5Rqd25? MUWyN|k1OTh|Mh?=
HuH7 NYrhPYx5TnWwY4Tpc44hSXO|YYm= MoT6OVAh|ryP Mlz5NlQhcA>? MUjEUXNQ NHHtSmJKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NVW4SFRoOjN7NEG4N|I>
SNU182 M2TpNmZ2dmO2aX;uJGF{e2G7 MmPsOVAh|ryP Mk\ZNlQhcA>? M1fQZ2ROW09? NGPMWJhKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MWeyN|k1OTh|Mh?=
SNU423 MljPSpVv[3Srb36gRZN{[Xl? NVzTNlJRPTBizszN M17hTFI1KGh? M4rLT2ROW09? M3PHb2lvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NESxZ4wzOzl2MUizNi=>

... Click to View More Cell Line Experimental Data

In vivo INCB018424 (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 in a JAK2V617F-driven mouse model. INCB018424 (180 mg/kg, orally, twice a day) markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model. [1] The primary end point is reached in 41.9% of patients in the Ruxolitinib group as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score. [2] A total of 28% of the patients in the Ruxolitinib (15 mg twice daily) group has at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis. [3]

Protocol

Kinase Assay:[1]
+ Expand

Binding assay:

Recombinant proteins are expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays use a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC50) is calculated as INCB018424 concentration required for inhibition of 50% of the fluorescent signal.
Cell Research:[1]
+ Expand
  • Cell lines: Ba/F3 and HEL cells
  • Concentrations: 3 μM
  • Incubation Time: 48 hours
  • Method: Cells are seeded at 2 × 103/well of white bottom 96-well plates, treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37 ℃ with 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: JAK2V617F-driven mouse model
  • Formulation: 5% dimethyl acetamide, 0.5% methocellulose
  • Dosages: 180 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/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 306.37
Formula

C17H18N6

CAS No. 941678-49-5
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01712659 Recruiting T Cell Leukemia, Adult|Leukemia, Adult T-Cell|T Cell Leukemia, HTLV I Associated National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) October 3, 2012 Phase 2
NCT02913261 Recruiting Corticosteroid Refractory Acute Graft vs Host Disease Novartis Pharmaceuticals|Novartis February 28, 2017 Phase 3
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT03012230 Not yet recruiting Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Mayo Clinic|National Cancer Institute (NCI) February 2017 Phase 1
NCT02928978 Not yet recruiting Ductal Carcinoma In Situ|Atypical Lobular Hyperplasia|Atypical Ductal Hyperplasia|Lobular Carcinoma In Situ Julie Nangia|Incyte Corporation|Translational Breast Cancer Research Consortium|Baylor Breast Care Center January 2017 Phase 2
NCT02966353 Not yet recruiting Primary Myelofibrosis (PMF)|Post-Polycythemia Vera-Myelofibrosis (PPV-MF)|Post-Essential Thrombocythemia Myelofibrosis (PET-MF) Novartis Pharmaceuticals|Novartis January 2017 Phase 2

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 S2902 and S1378 which seem to have same structure formula according to the product information?

  • Answer:

    These two chemicals are the two different chiral forms of Ruxolitinib. S2902 S-Ruxolitinib is the S form and S1378 Ruxolitinib is the D form. One of the carbon atoms in this molecule is asymmetric, making the two molecules mirror images of each other. The biological activities of these two molecules can be very different because of the confirmation differences.

  • Question 2:

    How about the half-life of the compound (Ruxolitinib)? How long is the duration of the inhibitory effect on JAK-STAT signaling?

  • Answer:

    The half-life of this compound in body is about 2~3 hours according to previous study. Generally, it is longer in vitro culture medium than in vivo. In paper, Ruxolitinib was also used for 24hours. http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=24711661.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID