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.

Size Price Stock Quantity  
In DMSO USD 208 In stock
USD 160 In stock
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USD 800 In stock

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Cited by 34 Publications

4 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.

     

    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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NHqydphMcW6jc3WgRZN{[Xl? NW\PeJdEOjBibXnu M1\ZdmROW09? NHTlTJRKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVCRLXnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxNu69VQ>? NWfiSlQxOjJ4OUiwPFQ>
TF1 NYLXNXY3U2mwYYPlJGF{e2G7 NXr1RZE5OjBibXnu M1\2XWROW09? NHzKc4xKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? NHXJT20zOjZ7OEC4OC=>
Human T cell NETMOWlMcW6jc3WgRZN{[Xl? M4flN2lvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyN:69VQ>? M{PUUVI{PTRyNkS4
Human monocyte MnrsT4lv[XOnIFHzd4F6 M2\qXWlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OILYP0bY12dGG2ZXSgV3RCXDWjIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOjcQvF2= NEexVFQzOzV2ME[0PC=>
Human monocyte MVzLbY5ie2ViQYPzZZk> M2rxSGlvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> MW[yN|U1ODZ2OB?=
HEL M4fZfWN6fG:2b4jpZ{BCe3OjeR?= M4DENVUh|ryP MmiyOFghcA>? NYnsdo1ZS3m2b4TvfIlkKGmwZHX4QVEzNjJn NX;rW2hJOjV7M{GzOFk>
SET-2 M1HKUGN6fG:2b4jpZ{BCe3OjeR?= NUXUVlhsPSEQvF2= NUC5T|BuPDhiaB?= MYjDfZRwfG:6aXOgbY5l\Xh;MUiuO{U> M2XyNFI2QTNzM{S5
HT93A NFzucJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfQbY44OzJyIH7N MkHSOUBl NEewcoVFVVOR MnXQTY5pcWKrdHnvckBw\iCJQ2OtSkBqdmS3Y3XkJIdz[W63bH;jfZRq[yCmaX\m[ZJmdnSrYYTpc44> NFj6XnozPThyNUm2Ni=>
CMK NVHPbG1jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H4ZWlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVU4OlZibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:w NUjCO2VMOjV|NUKxNlQ>
CMK NInTVGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLZeIpKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E3O0RibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjF4MzFOwG0> NGn3RZgzPTN3MkGyOC=>
CMK NV3RUZExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfnTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKFeWIFrBT{Bk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFc2KM7:TR?= MljUNlU{PTJzMkS=
NCI-H460 MoTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jLVWROW09? MnPJTWM2OD1yLkGzJO69VQ>? NYX6TZVrOjV{MUO2O|A>
NCI-H358 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPEUXNQ M2PpVWlEPTB;MD6xJO69VQ>? MYCyOVIyOzZ5MB?=
A549 NHKxVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\USG1UVw>? MnXjTWM2OD1yLkC0JO69VQ>? NWLEWGFzOjV{MUO2O|A>
A549/DDP Mn\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ny[2ROW09? NXeydGdTUUN3ME2wMlIzKM7:TR?= M2noVlI2OjF|Nkew
NCI-H1299 M{T1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTq[WhFVVOR NX7pXnFtUUN3ME2wMlI5KM7:TR?= M3XzSlI2OjF|Nkew
NCI-H2347 NIeyXmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHEZ4FYTE2VTx?= NXXIW3A5UUN3ME2wMlE4KM7:TR?= MXSyOVIyOzZ5MB?=
A549/DDP NHW4NppHfW6ldHnvckBCe3OjeR?= NVrMTmdZOzBibl2= MXe0PEBp MVTEUXNQ M4rOXGRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? NILydHEzPTJzM{[3NC=>
NCI-H1299 NIPJXWVHfW6ldHnvckBCe3OjeR?= M4exXVMxKG6P NF;4VJM1QCCq NWC2emdZTE2VTx?= NXfEPWhwTG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NGG4VoMzPTJzM{[3NC=>
NCI-H2347 MlfQSpVv[3Srb36gRZN{[Xl? M1rMdlMxKG6P M1vIUVQ5KGh? NEfMVFRFVVOR NGPsSGxF\WO{ZXHz[UBqdiCEY3yyJIV5eHKnc4Ppc44> NF;MWJYzPTJzM{[3NC=>
A549/DDP MV\BdI9xfG:|aYOgRZN{[Xl? MUizNEBvVQ>? M{j1blQ5KGh? NGP5OppFVVOR M1PtOGlv\HWldHnvckBw\iCjcH;weI9{cXN? M1L2V|I2OjF|Nkew
NCI-H1299 NX;Yb4hkSXCxcITvd4l{KEG|c3H5 NWSxRYpiOzBibl2= NYTzZmNNPDhiaB?= MnPCSG1UVw>? NWfsepliUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MmTYNlUzOTN4N{C=
NCI-H2347 NXHnNm56SXCxcITvd4l{KEG|c3H5 MmLuN|Ahdk1? NUjJfGo5PDhiaB?= MVXEUXNQ M1PFdWlv\HWldHnvckBw\iCjcH;weI9{cXN? MU[yOVIyOzZ5MB?=
Hep3B MXTGeY5kfGmxbjDBd5NigQ>? M4TifVEh|ryP Ml24NVYhcA>? NU[4TnpGTE2VTx?= M3jRc2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyCjY4TpeoUhW1SDVEOge4l1cCCLQ{WwJI9nKH53MDFOwG0> NInXc4YzPDVyMU[4PS=>
HepG2 NHS1SIZHfW6ldHnvckBCe3OjeR?= M3HVbFEh|ryP M1j3flE3KGh? NXjVeIJ7TE2VTx?= MX\JcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz M2nmb|I1PTBzNki5
Huh7 M1TldmZ2dmO2aX;uJGF{e2G7 NXeydGhWOSEQvF2= MYKxOkBp MkTHSG1UVw>? M2nCVGlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> NFzxXpYzPDVyMU[4PS=>
BaF3 MmT0T4lv[XOnIFHzd4F6 MYS4NEBvVQ>? MnziOkBp MYrEUXNQ NEj4bmlT\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2cEoGPURXQ2KGmwIFrBT|JXPjF5Rj3teZRifGWmIFLBSlMuTVCRUjDj[Yxt NUCxTFh3OjR{M{e3PVE>
DLD-1 NGjYdYRMcW6jc3WgRZN{[Xl? MkPWNlUh|ryP NEfVRo01QCCq Mor3SG1UVw>? MljqTY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= M4DMN|I1ODVyNUWw
RKO NG\PTmxMcW6jc3WgRZN{[Xl? Mn;6NlUh|ryP MonTOFghcA>? MUPEUXNQ MVjJcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w MnjpNlQxPTB3NUC=
DLD-1 MVvLbY5ie2ViQYPzZZk> MYmyOUDPxE1? MVi0PEBp MmjWSG1UVw>? MnjkTY5pcWKrdHnvckBw\iCMQVuyJJBpd3OyaH;yfYxifGmxbh?= NHz0ZWozPDB3MEW1NC=>
RKO NVzjSI9NU2mwYYPlJGF{e2G7 MUKyOUDPxE1? MlvwOFghcA>? NITVN2RFVVOR Mn;v[I9meyCwb4SgbY5pcWKrdDDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MXeyOFA2ODV3MB?=
DLD-1 M3XXXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPSSVE2OCEQvF2= MoKyOFghcA>? Mnr5SG1UVw>? MUXJR|UxRTF3LkWxJO69VQ>? MWeyOFA2ODV3MB?=
RKO NVLTcmdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3hOVAh|ryP NXzNWmRGPDhiaB?= MWjEUXNQ NXi5d5k{UUN3ME2xOE44PiEQvF2= MlHJNlQxPTB3NUC=
DLD-1 M2LPTWFxd3C2b4Ppd{BCe3OjeR?= MlrvNlUh|ryP MV[0PEBp NIHmeZBFVVOR NEfGNY9KdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= MlLTNlQxPTB3NUC=
RKO NWjPPFZtSXCxcITvd4l{KEG|c3H5 MWCyOUDPxE1? Mlz1OFghcA>? NEnud2xFVVOR MnHaTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? NHr1cJAzPDB3MEW1NC=>
HuH7 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XnV|UxKM7:TR?= M1jQW|Q5KGh? MWTEUXNQ MlHtQlgzLSC{ZXT1Z5Rqd25? M2TkbVI{QTRzOEOy
SNU182 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXXPWVNPTBizszN NXfMXWFmPDhiaB?= MWrEUXNQ M2rENV43PCVicnXkeYN1cW:w Mn33NlM6PDF6M{K=
SNU423 M4rnXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3W4T|UxKM7:TR?= M1rtelQ5KGh? MV;EUXNQ NY\pXZU1RjhzJTDy[YR2[3Srb36= NES0OIIzOzl2MUizNi=>
HuH7 MkK0SpVv[3Srb36gRZN{[Xl? NVz4boJTPTBizszN NESxbIgzPCCq MXfEUXNQ MorvTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M37z[|I{QTRzOEOy
SNU182 MXzGeY5kfGmxbjDBd5NigQ>? MmTSOVAh|ryP NIDS[|QzPCCq NFy4cnBFVVOR NX3SPXNMUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= MYiyN|k1OTh|Mh?=
SNU423 MljySpVv[3Srb36gRZN{[Xl? M{XseVUxKM7:TR?= Mlq1NlQhcA>? NYruVZVvTE2VTx?= MVzJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NVvJW|JVOjN7NEG4N|I>

... 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
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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
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  • 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
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  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02396628 Not yet recruiting Graft vs Host Disease Prof. Dr. Nikolas von Bubnoff|Clinical Trials Unit Freiburg|University Hospital Freiburg September 2016 Phase 2
NCT02784496 Not yet recruiting Myelofibrosis M.D. Anderson Cancer Center|Incyte Corporation August 2016 Phase 2
NCT02723994 Not yet recruiting B-cell Acute Lymphoblastic Leukemia Incyte Corporation|Childrens Oncology Group August 2016 Phase 2
NCT02718300 Not yet recruiting Myelofibrosis Incyte Corporation June 2016 Phase 2
NCT02713386 Not yet recruiting Fallopian Tube Carcinosarcoma|Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Neoplasm|High Grade Ovarian Serous Adenocarcinoma|Ovarian Carcinosarcoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Primary Peritoneal Serous Adenocarcinoma|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer NRG Oncology|National Cancer Institute (NCI) May 2016 Phase 1|Phase 2
NCT02598297 Recruiting Early Myelofibrosis With High Molecular Risk Mutations. Novartis Pharmaceuticals|Novartis February 2016 Phase 3

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