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

6 Customer Reviews

  • a, Phospho- and total STAT1 in MDA-MB-453 cells treated with abemaciclib with or without ruxolitinib for 7 days.

    Nature, 2017, 548(7668):471-475. Ruxolitinib (INCB018424) purchased from Selleck.

    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 NFfPcJVMcW6jc3WgRZN{[Xl? M17vZlIxKG2rbh?= NHy4RYdFVVOR MYnJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzMt88US=> M3zTblIzPjl6MEi0
TF1 MnLNT4lv[XOnIFHzd4F6 MmjwNlAhdWmw M{jJZWROW09? NHfmZ3RKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? NESxNYgzOjZ7OEC4OC=>
Human T cell NYLucZA3U2mwYYPlJGF{e2G7 NFjCZY1KdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? M4q4VlI{PTRyNkS4
Human monocyte MXPLbY5ie2ViQYPzZZk> NF;KS5VKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGdONUOVRj3zeIlufWyjdHXkJHNVSVR3YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODJ4zszN M3fNVlI{PTRyNkS4
Human monocyte M2\hN2tqdmG|ZTDBd5NigQ>? NUjNSnQ{UW6qaXLpeIlwdiCxZjDKRWszNzFiaX6gbJVu[W5ibX;uc4N6fGW|IHX4dJJme3OrbnegR2QyPCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmITnfhcY1iNXO2aX31cIF1\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCzNe69VQ>? M2P5XFI{PTRyNkS4
HEL NH3Ob|NEgXSxdH;4bYMhSXO|YYm= MlL6OUDPxE1? MlK1OFghcA>? MX\DfZRwfG:6aXOgbY5l\Xh;MUKuNkU> NULyNJdZOjV7M{GzOFk>
SET-2 MVfDfZRwfG:6aXOgRZN{[Xl? MnPXOUDPxE1? M3ryUlQ5KGh? NGr2[IhEgXSxdH;4bYMhcW6mZYi9NVgvPyV? MmTSNlU6OzF|NEm=
HT93A NI\KZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXoXHR5OzJyIH7N NITEPIU2KGR? MX7EUXNQ NUfuc4JbUW6qaXLpeIlwdiCxZjDHR3MuTiCrbnT1Z4VlKGe{YX71cI9kgXSrYzDkbYZn\XKnboTpZZRqd25? MYiyOVgxPTl4Mh?=
CMK M3PIeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G1O|JXKG23dHH0bY9vKGOnbHygdJJwdGmoZYLheIlwdg>? NHG4ZpAzPTN3MkGyOC=>
CMK M37afWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\NSopKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E3O0RibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjF4MzFOwG0> M3nl[FI2OzV{MUK0
CMK NF;NZo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWm5RYpMUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=> Ml3RNlU{PTJzMkS=
NCI-H460 M4PtRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP1SG1UVw>? NEjFSpJKSzVyPUCuNVMh|ryP MUSyOVIyOzZ5MB?=
NCI-H358 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWD4NVA1TE2VTx?= NVnyTZp[UUN3ME2wMlEh|ryP M2LGWlI2OjF|Nkew
A549 Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHlXJE3TE2VTx?= M{m3O2lEPTB;MD6wOEDPxE1? NXfpO|B[OjV{MUO2O|A>
A549/DDP MlmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUC4PFM3TE2VTx?= MUHJR|UxRTBwMkKg{txO M4\DUlI2OjF|Nkew
NCI-H1299 M132T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILQV5NFVVOR NFPTb|RKSzVyPUCuNlgh|ryP M3f5c|I2OjF|Nkew
NCI-H2347 NVXNdlJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vITGROW09? NVHPZlB6UUN3ME2wMlE4KM7:TR?= NUm5NHVzOjV{MUO2O|A>
A549/DDP MmD4SpVv[3Srb36gRZN{[Xl? MXizNEBvVQ>? MXm0PEBp NUnKeXpRTE2VTx?= NX30[2VLTG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MVqyOVIyOzZ5MB?=
NCI-H1299 M{PqfGZ2dmO2aX;uJGF{e2G7 M2q3blMxKG6P NFraNIw1QCCq NITncXZFVVOR NYrNVplrTG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NHrQdG4zPTJzM{[3NC=>
NCI-H2347 MVHGeY5kfGmxbjDBd5NigQ>? NHf3cXo{OCCwTR?= MWq0PEBp MXrEUXNQ M2jmUmRm[3KnYYPlJIlvKEKlbEKg[ZhxemW|c3nvci=> MWWyOVIyOzZ5MB?=
A549/DDP NFjTZVNCeG:ydH;zbZMhSXO|YYm= M17lZlMxKG6P NH7JTpo1QCCq NGPF[Y9FVVOR NImxcYFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NGrpbVgzPTJzM{[3NC=>
NCI-H1299 M37KdWFxd3C2b4Ppd{BCe3OjeR?= NGfuSo8{OCCwTR?= MXe0PEBp NXq1NXNsTE2VTx?= MUjJcoR2[3Srb36gc4Yh[XCxcITvd4l{ M3:1[|I2OjF|Nkew
NCI-H2347 MkHmRZBweHSxc3nzJGF{e2G7 NYHt[VRLOzBibl2= MV:0PEBp MXzEUXNQ Ml32TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NVu1R286OjV{MUO2O|A>
Hep3B M37GWmZ2dmO2aX;uJGF{e2G7 Mn\HNUDPxE1? NVzS[5J3OTZiaB?= NVrPVWJxTE2VTx?= NGi3NXVKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9iYXP0bZZmKFOWQWSzJJdqfGhiSVO1NEBw\iC-NUCg{txO NY\BelVrOjR3MEG2PFk>
HepG2 MX\GeY5kfGmxbjDBd5NigQ>? NF62N24yKM7:TR?= MYqxOkBp MVLEUXNQ NUjtXVlyUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MlTiNlQ2ODF4OEm=
Huh7 MU\GeY5kfGmxbjDBd5NigQ>? NHf6XGoyKM7:TR?= MV6xOkBp Mn3kSG1UVw>? NYHHWllRUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? NW\4NXFkOjR3MEG2PFk>
BaF3 MkXpT4lv[XOnIFHzd4F6 M{fobFgxKG6P M3S2VVYhcA>? MlrNSG1UVw>? M3rIW3Jm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\sLiU2TBWFUhcW5iSlHLNnY3OTeILX31eIF1\WRiQlHGN{1GWE:UIHPlcIw> NY\ZdWczOjR{M{e3PVE>
DLD-1 Mne3T4lv[XOnIFHzd4F6 NYfmdZRNOjVizszN NFPQZpA1QCCq NI\xVHJFVVOR MWTJcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w NVvpOZk1OjRyNUC1OVA>
RKO NGX6Z|hMcW6jc3WgRZN{[Xl? Mk\RNlUh|ryP NFHwbHY1QCCq NYjNcWFoTE2VTx?= M4fXeGlvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36= M3;1ZVI1ODVyNUWw
DLD-1 NH34WlJMcW6jc3WgRZN{[Xl? NWfQNHc4OjVizszN NYLBUpc{PDhiaB?= M4rGT2ROW09? NVXYOnZPUW6qaXLpeIlwdiCxZjDKRWszKHCqb4PwbI9zgWyjdHnvci=> NWDNOoNCOjRyNUC1OVA>
RKO NFHScndMcW6jc3WgRZN{[Xl? NITSdWozPSEQvF2= NYK4XoRsPDhiaB?= NEDkNnFFVVOR NWDWNJBR\G:nczDuc5QhcW6qaXLpeEBLSUtzIIDoc5NxcG:{eXzheIlwdg>? MlfXNlQxPTB3NUC=
DLD-1 NIDXSpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYi1NEDPxE1? MXe0PEBp MUjEUXNQ MmmyTWM2OD1zNT61NUDPxE1? NVPnS|ZiOjRyNUC1OVA>
RKO MmrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vsS|UxKM7:TR?= NV\WOXdYPDhiaB?= NGHUSVFFVVOR NHnYd3pKSzVyPUG0Mlc3KM7:TR?= NGXrW48zPDB3MEW1NC=>
DLD-1 MX\BdI9xfG:|aYOgRZN{[Xl? M2\XclI2KM7:TR?= MVm0PEBp MlnuSG1UVw>? NHK2XYlKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= NYHpXo0yOjRyNUC1OVA>
RKO MnH3RZBweHSxc3nzJGF{e2G7 NH\Sb3czPSEQvF2= M1HkelQ5KGh? NF35cW9FVVOR NWrONYFtUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= MXGyOFA2ODV3MB?=
HuH7 M{TlUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT5OVAh|ryP MoTNOFghcA>? M3L2SGROW09? NHfYTJA,QDJnIILl[JVkfGmxbh?= Mn7DNlM6PDF6M{K=
SNU182 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfmOVAh|ryP NHr3XlM1QCCq Mk\OSG1UVw>? MkLSQlY1LSC{ZXT1Z5Rqd25? MWOyN|k1OTh|Mh?=
SNU423 MkjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVr0TWR3PTBizszN MYm0PEBp MX7EUXNQ NWLIbJVQRjhzJTDy[YR2[3Srb36= MmXoNlM6PDF6M{K=
HuH7 MlHDSpVv[3Srb36gRZN{[Xl? M37pNVUxKM7:TR?= NVfuTHhpOjRiaB?= NEL2TYZFVVOR NYrxRmJSUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= M{TiSFI{QTRzOEOy
SNU182 NULU[JlrTnWwY4Tpc44hSXO|YYm= MmjNOVAh|ryP MUOyOEBp Ml[2SG1UVw>? MmXXTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M3eweVI{QTRzOEOy
SNU423 M2LxbWZ2dmO2aX;uJGF{e2G7 MmTiOVAh|ryP NG\JZ|gzPCCq MoLQSG1UVw>? M1rLNGlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NGr5OHEzOzl2MUizNi=>

... 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)
Ethanol 61 mg/mL (199.1 mM)
Water 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.

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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