Ruxolitinib (INCB018424)

For research use only.

Catalog No.S1378

350 publications

Ruxolitinib (INCB018424) Chemical Structure

CAS No. 941678-49-5

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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

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Selleck's Ruxolitinib (INCB018424) has been cited by 350 publications

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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. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
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
SNU423 MmqzSpVv[3Srb36gRZN{[Xl? M{LTOVUxKM7:TR?= M3zNNFI1KGh? M3XRZ2ROW09? MYTJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NHLOSVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 MYDGeY5kfGmxbjDBd5NigQ>? NVzTe3JzPTBizszN MmGyNlQhcA>? NIP5eJJFVVOR Ml\MTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M{m4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
HuH7 NE\Xb5ZHfW6ldHnvckBCe3OjeR?= NWDJOY0{PTBizszN MX2yOEBp MVXEUXNQ NIXZXGJKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NXfITmtoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU423 MnfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV21NEDPxE1? NHPUXZo1QCCq NYTXZWZuTE2VTx?= NE\GTIM,QDFnIILl[JVkfGmxbh?= M3;Y[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 NXTBcY1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rMd|UxKM7:TR?= MljsOFghcA>? Mk\pSG1UVw>? MVG+OlQmKHKnZIXjeIlwdg>? NELoWlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;hdlA2OCEQvF2= MonqOFghcA>? NFS4dWdFVVOR MmHRQlgzLSC{ZXT1Z5Rqd25? M2DtVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
RKO MXfBdI9xfG:|aYOgRZN{[Xl? MoXaNlUh|ryP NEnUbGQ1QCCq NXPZNnM4TE2VTx?= Mli5TY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? NH7mUmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 MmXORZBweHSxc3nzJGF{e2G7 MlrDNlUh|ryP Mn;1OFghcA>? MVfEUXNQ M2ryfWlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| NU\zd5dpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
DLD-1 NWK5XohRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkH3OVAh|ryP M3zOWVQ5KGh? MoDaSG1UVw>? NEXid|dKSzVyPUG1MlUyKM7:TR?= Mnf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
RKO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TsSVUxKM7:TR?= NF7SdZE1QCCq MlniSG1UVw>? M4HVd2lEPTB;MUSuO|Yh|ryP M3zo[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MUfLbY5ie2ViQYPzZZk> M4jBdVI2KM7:TR?= NV;rPYszPDhiaB?= NWXTW|NpTE2VTx?= MVnkc4V{KG6xdDDpcohq[mm2IFrBT|EheGixc4Doc5J6dGG2aX;u MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NUPM[XhMU2mwYYPlJGF{e2G7 NInaNIQzPSEQvF2= MmT2OFghcA>? NXjxXHhTTE2VTx?= NUXPbG1bUW6qaXLpeIlwdiCxZjDKRWszKHCqb4PwbI9zgWyjdHnvci=> NWHFPFNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO MVzLbY5ie2ViQYPzZZk> NHu3OI0zPSEQvF2= M3TXWFQ5KGh? M4\NR2ROW09? NITzWZpKdmirYnn0bY9vKG:oIFrBT|EheGixc4Doc5J6dGG2aX;u Ml\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 MVzLbY5ie2ViQYPzZZk> MX:yOUDPxE1? MVG0PEBp NXXoOGxGTE2VTx?= NHTBUlJKdmirYnn0bY9vKG:oIFrBT|EheGixc4Doc5J6dGG2aX;u M{jhNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
BaF3 MUDLbY5ie2ViQYPzZZk> NX\MfHBQQDBibl2= NFW2WXg3KGh? MnHWSG1UVw>? MVjS[YR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gc4bDqFOWQWS1JIlvKEqDS{LWOlE4Ti2vdYTheIVlKEKDRkOtSXBQWiClZXzs M{nOT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkO3O|kyLz5{NEKzO|c6OTxxYU6=
Huh7 MnO4SpVv[3Srb36gRZN{[Xl? M{foZ|Eh|ryP MUmxOkBp NWX1WHFGTE2VTx?= NVjrWZdIUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? NHHtcIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
HepG2 MoTRSpVv[3Srb36gRZN{[Xl? M2\WSlEh|ryP M4nxelE3KGh? NIPyUmdFVVOR M2\5S2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> NIi2O3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
Hep3B MVPGeY5kfGmxbjDBd5NigQ>? M{DwN|Eh|ryP MnXsNVYhcA>? NFGzTWhFVVOR NHiyNW1KdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9iYXP0bZZmKFOWQWSzJJdqfGhiSVO1NEBw\iC-NUCg{txO MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
NCI-H2347 MWnBdI9xfG:|aYOgRZN{[Xl? MkfsN|Ahdk1? NYLPZYpWPDhiaB?= MVrEUXNQ NXrpWJF3UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 MVfBdI9xfG:|aYOgRZN{[Xl? MVGzNEBvVQ>? NVTVeHR4PDhiaB?= NEXvbolFVVOR NFnvPYlKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NXf3[YcyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP NF\zZXhCeG:ydH;zbZMhSXO|YYm= NXfXUpQ1OzBibl2= M1zD[lQ5KGh? NEnRcWpFVVOR NGrtVlFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| Mn61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H1299 NG\ue4ZHfW6ldHnvckBCe3OjeR?= NF3SPWI{OCCwTR?= Ml21OFghcA>? M4j2NGROW09? M{nleGRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? NU\jNWhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H2347 Mn7tSpVv[3Srb36gRZN{[Xl? NGjVRZo{OCCwTR?= NWK4eJZFPDhiaB?= NEHnVmlFVVOR NFPudJpF\WO{ZXHz[UBqdiCEY3yyJIV5eHKnc4Ppc44> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP MlPYSpVv[3Srb36gRZN{[Xl? M37SfVMxKG6P M1vpSVQ5KGh? Mnq1SG1UVw>? MlHpSI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? M{LKSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPqeGFTTE2VTx?= MWjJR|UxRTBwMUeg{txO NH7yRWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknrSG1UVw>? NIrGdW1KSzVyPUCuNlgh|ryP NUPzW3V2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP M4C0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDEUXNQ NHXEdVhKSzVyPUCuNlIh|ryP MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549 M1vQcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjEUXNQ NH7TTVRKSzVyPUCuNFQh|ryP MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H358 M4Pj[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLFfYxFVVOR NIi3VpZKSzVyPUCuNUDPxE1? Mon0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H460 M1;rTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnuPGVXTE2VTx?= M2S2O2lEPTB;MD6xN{DPxE1? NIrPZmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
CMK M{PheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhX1RiSlHLJINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiMD6wO|Uh|ryP NVHidlQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
CMK NW[zTFZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXHOYNtUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPjOGIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zNkOg{txO NX7Ce|ByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
CMK NVzJUmppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHCTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOVczXiCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25? NYPuU5lZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
HT93A Mo[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWizNlAhdk1? NEX3OVc2KGR? MWrEUXNQ NU\uT|FSUW6qaXLpeIlwdiCxZjDHR3MuTiCrbnT1Z4VlKGe{YX71cI9kgXSrYzDkbYZn\XKnboTpZZRqd25? NYrLRo5MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NFU6PjJpPkK1PFA2QTZ{PD;hQi=>
SET-2 MVHDfZRwfG:6aXOgRZN{[Xl? MVe1JO69VQ>? MWK0PEBp NYHTPZVYS3m2b4TvfIlkKGmwZHX4QVE5Njdn M3HTd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
HEL NV\tT2tFS3m2b4TvfIlkKEG|c3H5 Mn7xOUDPxE1? MnLYOFghcA>? MVjDfZRwfG:6aXOgbY5l\Xh;MUKuNkU> MlHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{GzOFkoRjJ3OUOxN|Q6RC:jPh?=
Human monocyte MXvLbY5ie2ViQYPzZZk> NHG1bZVKdmirYnn0bY9vKG:oIFrBT|IwOSCrbjDoeY1idiCvb37vZ5l1\XNiZYjwdoV{e2mwZzDDSFE1KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUU[QZ3HtcYEue3SrbYXsZZRm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEOx{txO M3LaS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
Human monocyte M2HjfGtqdmG|ZTDBd5NigQ>? NX\SeVNFUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBIVS2FU1[td5RqdXWuYYTl[EBUXEGWNXGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{Nt88US=> MoH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human T cell NVzaS251U2mwYYPlJGF{e2G7 NFHxW2pKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? MojoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
TF1 M1fHVmtqdmG|ZTDBd5NigQ>? NXzTTJdbOjBibXnu NHftfFFFVVOR MlPYTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkVOwG0> NEDLc|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
TF1 M3Hl[GtqdmG|ZTDBd5NigQ>? M{HRb|IxKG2rbh?= MkXRSG1UVw>? MXHJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzMt88US=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
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SET2 cells M{frbWpCUyCrbnjpZol1cW:wIHHzd4F6 NXnDUVBtUUN3MDC9JFAvODBzOESg{txO M1PqflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|ME[xOlYxLz5{M{C2NVY3ODxxYU6=
Sf21 cells NWL5[oV5UkGNIHnubIljcXSrb36gZZN{[Xl? M3H1fVEhcA>? NGrHWG9KSzVyIE2gNE4xODJ6IN88US=> MoPRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3OUG0NFIoRjJ{NUmxOFAzRC:jPh?=
Sf21 cells NH7PelJLSUtiaX7obYJqfGmxbjDhd5NigQ>? MVS2NEBucW5? M2TocWlEPTBiPTCwMlAxOyEQvF2= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|N{O1PUc,OjdzM{ezOVk9N2F-
Sf9 cells MmjzTmFMKGmwaHnibZRqd25iYYPzZZk> NGLpZ44yKGh? Ml;ZT4khRSByLkCwN|Ih|ryP MlrsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4Nki0PFQoRjJ|Nk[4OFg1RC:jPh?=
Sf21 cells NFjNTXhLSUtiaX7obYJqfGmxbjDhd5NigQ>? MXqxJIg> MXnJR|UxKD1iMD6wNFM{KM7:TR?= NFHndVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
TF1 cells MofGTmFMKGmwaHnibZRqd25iYYPzZZk> NHe4V|Y{OCCvaX6= NWLUTmZoUUN3MDC9JFAvODB4OEWg{txO MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB4MU[2NEc,OjNyNkG2OlA9N2F-
CD34+ cells MlyyTmFMKGmwaHnibZRqd25iYYPzZZk> MUHJR|UxKD1iMD6wNFgh|ryP M{PETVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
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T cells MoHNTmFMKGmwaHnibZRqd25iYYPzZZk> MorjTWM2OCB;IECuNFI{KM7:TR?= MmjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
T cells M2W4PWpCUyCrbnjpZol1cW:wIHHzd4F6 NX73RVNsUUN3MDC9JFAvODJ|IN88US=> M{GyV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
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T cells MWfKRWshcW6qaXLpeIlwdiCjc4PhfS=> MlHZTWM2OCB;IECuNFMyKM7:TR?= M1zOOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells NIPZ[GxLSUtiaX7obYJqfGmxbjDhd5NigQ>? M3r4dGlEPTBiPTCwMlA{OSEQvF2= Mk\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
PBMC cells M4i4c2pCUyCrbnjpZol1cW:wIHHzd4F6 MnHyTWM2OCB;IECuNFQh|ryP NXXUcHJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5Nlc1OjNpPkK2PVI4PDJ|PD;hQi=>
Sf21 cells M1vTVGpCUyCrbnjpZol1cW:wIHHzd4F6 NUjFW4tNOSCq NFvpSoZKSzVyIE2gNE41OjhizszN M3;rWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUmxOFAzLz5{MkW5NVQxOjxxYU6=
PBMC cells NH7pWnVUXEGWNTDpcohq[mm2aX;uJIF{e2G7 M2C3XGlEPTBiPTCwMlQ1QCEQvF2= MnzKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
CD34+ cells NFjz[4VLSUtiaX7obYJqfGmxbjDhd5NigQ>? MnjvOFUhdWmw NYnzNGx[UUN3MDC9JFAvPjd5IN88US=> NXn5WVQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2OzNpPkK0OFE4PTN|PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cleaved PARP / cleaved caspase3; 

PubMed: 29849942     


OVCAR-8 and MDAH 2774 cells were incubated with various concentrations of ruxolitinib for 48 h. Apoptosis was determined by using cleaved poly-ADP ribose polymerase (PARP) and cleaved caspase-3 by Western blot.

p-JAK2 / p-AKT / p-MAPK / Bcl-xl / MCL-1; 

PubMed: 29849942     


OVCAR-8 and MDAH2774 cells were treated with ruxolitinib (20 μM), paclitaxel (10 nM) or the combination for 24 h. Whole cells were collected and determined for the change of STAT3, AKT and ERK pathways and expression of BCL-XL and MCL-1 by Western blot.

c-Myc / c-Jun / Cyclin B / Cyclin D / Bcl-2 / HIF-1α; 

PubMed: 30930994     


Effects of ruxolitinib on the expression of downstream target genes of the JAK-STAT pathway. The protein levels of c-Myc, c-Jun, Cyclin B1, Cyclin D1, Bcl-2 and HIF-1α were determined in MCF-7 and TAMR-MCF-7 cells 24 h following ruxolitinib treatment (0.1-10 μM). 

p-STAT3; 

PubMed: 29849942     


Dose-dependent inhibition of STAT3 phosphorylation. Human ovarian cancer cells, OVCAR-8, MDAH2774, and SKOV3, were treated with the indicated concentrations of ruxolitinib for 24 h. Phosphorylation of STAT3 was analyzed by Western blot. 

29849942 30930994
Growth inhibition assay
Cell viability; 

PubMed: 29849942     


Dose dependent inhibition of cell viability. Human ovarian cancer cell lines were treated with the indicated concentrations of ruxolitinib. Cell viability was determined 72 h later. The IC50 was determined by the Chou-Talalay method. *P<0.05; ***P<0.0005, ruxolitinib vs control in OVCAR-8 cells; #P<0.05; ##P<0.005; ###P<0.0005, ruxolitinib vs control in SKOV-3 cells; ^^P<0.005; ^^^P<0.0005, ruxolitinib vs control in MDAH2774 cells.

Cell apoptosis; 

PubMed: 29849942     


OVCAR-8 and MDAH 2774 cells were incubated with various concentrations of ruxolitinib for 48 h. Apoptosis was determined by flow cytometry using annexin V and PI staining.

Cell proliferation; 

PubMed: 29515770     


Cells were plated into 48 well plates and cell growth was measured every 48 hours via MTS assay following ruxolitinib treatment (0, 1, 10 and 100 uM) in L-428 (left) and HDLM-2 (middle) HL cells, and Karpas-1106P PMBL cells (right).

29849942 29515770
Immunofluorescence
α-tubulin; 

PubMed: 26356819     


Confocal analysis of HEL cells, treated or not with different concentration of ruxolitinib (100 and 300 nM), displaying α-Tubulin (green) and DAPI (blue) staining; MERGE shows the overlapped images. Scale bars are shown in the figure (10 μm). Note more diffuse microtubule networks in ruxolutinib-treated cells.

26356819
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]
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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:[1]
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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:[1]
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  • Animal Models: JAK2V617F-driven mouse model
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
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
in solvent
Synonyms N/A
Smiles C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04543279 Not yet recruiting Drug: Fostamatinib|Drug: Ruxolitinib Myelofibrosis Washington University School of Medicine|Rigel Pharmaceuticals January 31 2021 Phase 2
NCT04551131 Not yet recruiting Drug: Ruxolitinib|Drug: Dexamethasone|Drug: Etoposide Hemophagocytic Lymphohistiocytosis St. Jude Children''s Research Hospital|Incyte Corporation|North American Consortium for Histiocytosis January 2021 Phase 1|Phase 2
NCT04485260 Recruiting Drug: KRT-232|Drug: Ruxolitinib Myelofibrosis Kartos Therapeutics Inc. December 2020 Phase 1|Phase 2
NCT04454658 Recruiting Drug: ABBV-744|Drug: Navitoclax|Drug: Ruxolitinib Myelofibrosis (MF) AbbVie August 19 2020 Phase 1|Phase 2
NCT04359290 Active not recruiting Drug: Ruxolitinib administration ARDS Human|COVID Philipps University Marburg Medical Center July 1 2020 Phase 2
NCT04480086 Not yet recruiting Drug: Mivebresib|Drug: Navitoclax|Drug: Ruxolitinib Myelofibrosis (MF) AbbVie July 31 2020 Phase 1

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

If you have any other enquiries, please leave a message.

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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