Ruxolitinib (INCB018424)

Catalog No.S1378

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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Ruxolitinib (INCB018424) Chemical Structure

Ruxolitinib (INCB018424) Chemical Structure
Molecular Weight: 306.37

Validation & Quality Control

Cited by 34 publications:

4 customer reviews :

Quality Control & MSDS

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Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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TF1MUfLbY5ie2ViQYPzZZk>MlzMNlAhdWmwM4LhXGROW09?MYDJcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWw3NWmwZIXj[YQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{NN88US=>M4D3fFIzPjl6MEi0
Human T cellMXnLbY5ie2ViQYPzZZk>M3Hxe2lvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyN:69VQ>?MnPQNlM2PDB4NEi=
Human monocyteNFH3ZldMcW6jc3WgRZN{[Xl?MXvJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI3|ryPMmTMNlM2PDB4NEi=
Human monocyteMY\LbY5ie2ViQYPzZZk>MoXuTY5pcWKrdHnvckBw\iCMQVuyM|EhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlHVmejbX3hMZN1cW23bHH0[YQhW1SDVEGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB|Md88US=>NGrUXZAzOzV2ME[0PC=>
HELM{X5SmN6fG:2b4jpZ{BCe3OjeR?=M4fXdVUh|ryPNVe1bXNFPDhiaB?=NWLGT3BVS3m2b4TvfIlkKGmwZHX4QVEzNjJnNIfHfoczPTl|MUO0PS=>
SET-2M4PoZ2N6fG:2b4jpZ{BCe3OjeR?=MnHsOUDPxE1?MYi0PEBpNWXxd49NS3m2b4TvfIlkKGmwZHX4QVE5NjdnM4jDelI2QTNzM{S5
HT93AM4LYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUPaTWJ[OzJyIH7NM4\STFUh\A>?M{fpUWROW09?NFrqT2hKdmirYnn0bY9vKG:oIFfDV{1HKGmwZIXj[YQh\3KjboXsc4N6fGmlIHTp[oZmemWwdHnheIlwdg>?M2rhVFI2QDB3OU[y
CMKM2LWTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUTJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G1O|JXKG23dHH0bY9vKGOnbHygdJJwdGmoZYLheIlwdg>?NIW1[40zPTN3MkGyOC=>
CMKNHq4[mtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGP0[lBKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E3O0RibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjF4MzFOwG0>M4TCXVI2OzV{MUK0
CMKNIHzWVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NX\5PGZMUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=>MV:yOVM2OjF{NB?=
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NCI-H358NXzEb5d7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MX\EUXNQMUjJR|UxRTBwMTFOwG0>M1nBclI2OjF|Nkew
A549NIj3eHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NUDmTId[TE2VTx?=NYTS[FhzUUN3ME2wMlA1KM7:TR?=MUOyOVIyOzZ5MB?=
A549/DDPMXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1LGVWROW09?NWnpNJlMUUN3ME2wMlIzKM7:TR?=MnW2NlUzOTN4N{C=
NCI-H1299M1rH[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFrEcXRFVVORMoD4TWM2OD1yLkK4JO69VQ>?MmPKNlUzOTN4N{C=
NCI-H2347MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXfEb5VQTE2VTx?=MonxTWM2OD1yLkG3JO69VQ>?MViyOVIyOzZ5MB?=
A549/DDPNUPTOXZ4TnWwY4Tpc44hSXO|YYm=MnXpN|Ahdk1?MVy0PEBpM4PWOWROW09?Ml76SI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>?MkTVNlUzOTN4N{C=
NCI-H1299M3:yPWZ2dmO2aX;uJGF{e2G7NVvEbHhkOzBibl2=Mn7ZOFghcA>?M{jMR2ROW09?NHfGZplFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wMXWyOVIyOzZ5MB?=
NCI-H2347M3n5SmZ2dmO2aX;uJGF{e2G7M4rK[lMxKG6PMlPmOFghcA>?NFf3cZlFVVORNXWzOmhyTGWlcnXhd4UhcW5iQnPsNkBmgHC{ZYPzbY9vNYPqTmZEOjV{MUO2O|A>
A549/DDPMn\uRZBweHSxc3nzJGF{e2G7MXOzNEBvVQ>?Mk\POFghcA>?NE\5[W1FVVORNEfWblNKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|MoH6NlUzOTN4N{C=
NCI-H1299Mn7QRZBweHSxc3nzJGF{e2G7MmDWN|Ahdk1?MYS0PEBpMkTsSG1UVw>?M37GRWlv\HWldHnvckBw\iCjcH;weI9{cXN?NXW2U5lYOjV{MUO2O|A>
NCI-H2347NGW4PGJCeG:ydH;zbZMhSXO|YYm=NX7KNYxTOzBibl2=MVq0PEBpNXLUbWdoTE2VTx?=NUfxOHlJUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?=M{jucFI2OjF|Nkew
Hep3BM4LBfWZ2dmO2aX;uJGF{e2G7M3TMZVEh|ryPMX2xOkBpNYPZOFhQTE2VTx?=MkH3TY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKGGldHn2[UBUXEGWMzD3bZRpKEmFNUCgc4YhhjVyIN88US=>NYT3RXYyOjR3MEG2PFk>
HepG2MkW2SpVv[3Srb36gRZN{[Xl?MkXWNUDPxE1?NWHVe2NjOTZiaB?=MmPISG1UVw>?NXTOVZc4UW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>?M{mzU|I1PTBzNki5
Huh7NYPpbGNmTnWwY4Tpc44hSXO|YYm=MVGxJO69VQ>?NVu0XYdTOTZiaB?=NG\jbFdFVVORM4rFN2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM>MoK3NlQ2ODF4OEm=
BaF3MnrUT4lv[XOnIFHzd4F6MW[4NEBvVQ>?MVK2JIg>M4XlbWROW09?NW\mTJMxWmWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:owrDTWGFVPSCrbjDKRWszXjZzN1[tcZV1[XSnZDDCRWY{NUWST2KgZ4VtdA>?NVjUTVVXOjR{M{e3PVE>
DLD-1MVTLbY5ie2ViQYPzZZk>MXSyOUDPxE1?Mn\0OFghcA>?M3XpbWROW09?M3LST2lvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36=MnHQNlQxPTB3NUC=
RKOMWjLbY5ie2ViQYPzZZk>NXP1UZNWOjVizszNNIqwRXM1QCCqMY\EUXNQMoKwTY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?=MmPoNlQxPTB3NUC=
DLD-1NUnkNWhsU2mwYYPlJGF{e2G7NVzJZXdCOjVizszNM{mxRVQ5KGh?NFHyfHJFVVORMWLJcohq[mm2aX;uJI9nKEqDS{KgdIhwe3Cqb4L5cIF1cW:wMYmyOFA2ODV3MB?=
RKONWjvNHNkU2mwYYPlJGF{e2G7NU\sUFlQOjVizszNMn7mOFghcA>?NIfZTm5FVVORNXzaZZJY\G:nczDuc5QhcW6qaXLpeEBLSUtzIIDoc5NxcG:{eXzheIlwdg>?NFrlXXYzPDB3MEW1NC=>
DLD-1NW\jNHBXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MYm1NEDPxE1?MkD1OFghcA>?MVTEUXNQMlflTWM2OD1zNT61NUDPxE1?MU[yOFA2ODV3MB?=
RKOM3\mNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF\OdIU2OCEQvF2=NXS3NVI{PDhiaB?=MlLQSG1UVw>?Ml3aTWM2OD1zND63OkDPxE1?NGnPeY0zPDB3MEW1NC=>
DLD-1NGLaOWZCeG:ydH;zbZMhSXO|YYm=M3LwSlI2KM7:TR?=MY[0PEBpNGDoNJpFVVORMYDJcoR2[2W|IHHwc5B1d3OrczDifUBi[3SrdnH0bY5oKGOjc4Dhd4UhOw>?NEj3bIQzPDB3MEW1NC=>
RKOM2nON2Fxd3C2b4Ppd{BCe3OjeR?=M2W2XFI2KM7:TR?=NHjwWoM1QCCqMXvEUXNQNEj2UG1KdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?=MViyOFA2ODV3MB?=
HuH7MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGj3[ZE2OCEQvF2=NITJSXo1QCCqMmrHSG1UVw>?NWLhRWJTRjh{JTDy[YR2[3Srb36=MWqyN|k1OTh|Mh?=
SNU182NUXCVWJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkjjOVAh|ryPMWC0PEBpMWrEUXNQNVraWHJzRjZ2JTDy[YR2[3Srb36=MWiyN|k1OTh|Mh?=
SNU423MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWe1NEDPxE1?NXjrdG9LPDhiaB?=MWfEUXNQM4r4Tl45OSVicnXkeYN1cW:wMnj6NlM6PDF6M{K=
HuH7M2\2c2Z2dmO2aX;uJGF{e2G7MVy1NEDPxE1?MYOyOEBpMoSzSG1UVw>?MlzqTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl?MY[yN|k1OTh|Mh?=
SNU182NGPkVG9HfW6ldHnvckBCe3OjeR?=M3zVV|UxKM7:TR?=M1PlflI1KGh?MWjEUXNQM33KNmlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7MUOyN|k1OTh|Mh?=
SNU423M3\RRmZ2dmO2aX;uJGF{e2G7NITzRXo2OCEQvF2=NYPUWWxPOjRiaB?=MWTEUXNQMV7Jcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>?MVqyN|k1OTh|Mh?=

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [1]

Animal Models JAK2V617F-driven mouse model
Formulation 5% dimethyl acetamide, 0.5% methocellulose
Dosages 180 mg/kg
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Quintas-Cardama A, et al. Blood, 2010, 115(15), 3109-3117.

[2] Verstovsek S, et al. N Engl J Med, 2012, 366(9), 799-807.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

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 Freibu  ...more 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|Hi  ...more 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

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Chemical Information

Download Ruxolitinib (INCB018424) SDF
Molecular Weight (MW) 306.37
Formula

C17H18N6

CAS No. 941678-49-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 61 mg/mL (199.1 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name (3R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Customer Product Validation(4)


Click to enlarge
Rating
Source Blood 2014 123(24), 3832-42. Ruxolitinib (INCB018424) purchased from Selleck
Method Flow cytometry
Cell Lines CD4<sup>+</sup> T cells
Concentrations 0-1 uM
Incubation Time 24 h
Results As shown in figure, STAT3 phosphorylation was significantly reduced when ruxolitinib exposed CD4+ T cells.

Click to enlarge
Rating
Source J Immunol 2012 189(6), 2784-92. Ruxolitinib (INCB018424) purchased from Selleck
Method Immunoblotting
Cell Lines BMDMs
Concentrations 0-1 uM
Incubation Time 1 h
Results To determine the concentrationof Ruxolitinib required to inhibit JAKs in macrophages, BMDMs were stimulated with IFN-β in the presence of various concentrations of Ruxolitinib. Ruxolitinib was required to compeletely block IFN-β–induced STAT1 phosphorylation in cells.

Click to enlarge
Rating
Source Gene Ther 2014 10.1038/gt.2014.83. Ruxolitinib (INCB018424) purchased from Selleck
Method VA7 infection assay
Cell Lines CT26LacZ, CT26WT cells
Concentrations 1 uM
Incubation Time 48 h
Results CT26LacZ cells were infected at low multiplicity of infection (MOI) (10 plaque-forming units (PFUs) per 50000 cells) by 48 h post infection (p.i.), the same virus dose in CT26WT cells resulted in a self-limiting infection that could only be rescued using JAK/STAT pathway inhibitor Ruxolitinib. Ruxolitinib enhanced the infection even further when the cells received small dose IFNβ pretreatment, an unanticipated synergetic effect we are currently investigating.

Click to enlarge
Rating
Source Yong Weon Yi Georgetown University. Ruxolitinib (INCB018424) purchased from Selleck
Method Western Blot
Cell Lines HS578T cells
Concentrations 0-3 μM
Incubation Time 18 h
Results INCB018424 treatment resulted in a reduction of STAT3 phosphorylation in a concentration-dependent manner.

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.

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.

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  • AZD1480

    AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

  • Fedratinib (SAR302503, TG101348)

    Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.

  • Momelotinib (CYT387)

    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.

  • WP1066

    WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1.

    Features:Similar to its parent compound AG490, WP1066 inhibits the phosphorylation of JAK2, but unlike AG490, WP1066 also degraded JAK2 protein.

  • Baricitinib (LY3009104, INCB028050)

    Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

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I want to use Ruxolitinib in a series of animal studies. We previously did a pilot study and were having problems solubilizing Rux. We tried putting the inhibitor in chromophore ethanol, but that ...

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You can prepare the stock solution of Ruxolitinib with DMSO and then dilute it with the vehicle (5% dimethyl acetamide, 0.5% carboxyl methylcellulose). This solution can be used for oral gava...

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