Ruxolitinib (INCB018424)

For research use only.

Catalog No.S1378

405 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.

Selleck's Ruxolitinib (INCB018424) has been cited by 405 publications

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. 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 NEXabVZHfW6ldHnvckBCe3OjeR?= Mn;oOVAh|ryP NEnQfHUzPCCq MW\EUXNQ MYXJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NXXGc2dYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU182 NIL3SW9HfW6ldHnvckBCe3OjeR?= M4faOFUxKM7:TR?= MlLzNlQhcA>? NWXSXXB5TE2VTx?= NEn6NpBKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= M2Di[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
HuH7 MUfGeY5kfGmxbjDBd5NigQ>? M4PNTVUxKM7:TR?= NEHYR5QzPCCq NV\YcFRxTE2VTx?= NXrqSYpnUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NEn6OXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU423 NGTnbZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVL0enc1PTBizszN NF;wdFc1QCCq NHTqS5JFVVOR NUPZXpVJRjhzJTDy[YR2[3Srb36= Ml7WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
SNU182 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nSSVUxKM7:TR?= NIP3S2o1QCCq NEPMOVVFVVOR NHn5eHk,PjRnIILl[JVkfGmxbh?= M2no[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
HuH7 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3MUW9sPTBizszN NGDWbIU1QCCq NXX6[21iTE2VTx?= M4TyeV45OiVicnXkeYN1cW:w MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
RKO MmPvRZBweHSxc3nzJGF{e2G7 NWSyPHpROjVizszN Mk\COFghcA>? MUjEUXNQ M4TFSGlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| MornQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 MlO0RZBweHSxc3nzJGF{e2G7 MV6yOUDPxE1? M{fPd|Q5KGh? NEnQU5RFVVOR M2DiSWlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknYOVAh|ryP NF;jU|U1QCCq MlPkSG1UVw>? MkfETWM2OD1zNT61NUDPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
RKO MlzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HUOVUxKM7:TR?= NIHoOFg1QCCq M3PzWGROW09? NVrvUlk1UUN3ME2xOE44PiEQvF2= M{LB[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MX;LbY5ie2ViQYPzZZk> NWL3OGpJOjVizszN MV20PEBp MnXQSG1UVw>? NXzyUINy\G:nczDuc5QhcW6qaXLpeEBLSUtzIIDoc5NxcG:{eXzheIlwdg>? NIK1eHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 MWPLbY5ie2ViQYPzZZk> NWPmU5pROjVizszN Mk[2OFghcA>? NEjj[llFVVOR NGLOXG1KdmirYnn0bY9vKG:oIFrBT|IheGixc4Doc5J6dGG2aX;u M3;MR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO NGe5N2tMcW6jc3WgRZN{[Xl? M3nZSlI2KM7:TR?= NH:yeHg1QCCq MnLMSG1UVw>? NYq5[mRVUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NInwN5NMcW6jc3WgRZN{[Xl? M3LjWVI2KM7:TR?= MljvOFghcA>? MUDEUXNQ Mo\lTY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= M3i4W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
BaF3 NYTjNmNOU2mwYYPlJGF{e2G7 M4jkNlgxKG6P MmTiOkBp MWPEUXNQ NES2PXVT\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2cEoGPURXQ2KGmwIFrBT|JXPjF5Rj3teZRifGWmIFLBSlMuTVCRUjDj[Yxt MnPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{M{e3PVEoRjJ2MkO3O|kyRC:jPh?=
Huh7 NYjzUI5GTnWwY4Tpc44hSXO|YYm= MlvQNUDPxE1? NXm0OZA4OTZiaB?= MVHEUXNQ MVLJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz NWT4cm9GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFE3QDlpPkK0OVAyPjh7PD;hQi=>
HepG2 M4jsS2Z2dmO2aX;uJGF{e2G7 M{nIVlEh|ryP MYSxOkBp MUXEUXNQ M{G1NmlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
Hep3B NIqwT4NHfW6ldHnvckBCe3OjeR?= M2LX[|Eh|ryP MUOxOkBp MV3EUXNQ M2TiPWlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyCjY4TpeoUhW1SDVEOge4l1cCCLQ{WwJI9nKH53MDFOwG0> Mk\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEG2PFkoRjJ2NUCxOlg6RC:jPh?=
NCI-H2347 M4rCT2Fxd3C2b4Ppd{BCe3OjeR?= MnLNN|Ahdk1? NFnHZ|U1QCCq NYniNHNmTE2VTx?= NXnpSoV2UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MknFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H1299 MX7BdI9xfG:|aYOgRZN{[Xl? MUKzNEBvVQ>? NXTMdmZ7PDhiaB?= M3;0bWROW09? NWTaUW8{UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M1fNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP MULBdI9xfG:|aYOgRZN{[Xl? NXi4Nnh{OzBibl2= Mnn6OFghcA>? MU\EUXNQ MVzJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MlvEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H1299 M1zpbGZ2dmO2aX;uJGF{e2G7 NYrOe4pROzBibl2= MVu0PEBp MWTEUXNQ NHf0Z|BFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w NF\qRmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H2347 NHXRblVHfW6ldHnvckBCe3OjeR?= M1z5blMxKG6P M4GydlQ5KGh? MXfEUXNQ NHTiZnBF\WO{ZXHz[UBqdiCEY3yyJIV5eHKnc4Ppc44> NGewUW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP NFjlcmRHfW6ldHnvckBCe3OjeR?= NGLWRXc{OCCwTR?= NWezXHRWPDhiaB?= MX3EUXNQ NYjjXpF{TG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= M1K3W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 NEHiRYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG1cVBFVVOR MVjJR|UxRTBwMUeg{txO M4CyTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 NYOxNVhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rFc2ROW09? NHH2OHJKSzVyPUCuNlgh|ryP M2q2RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHwcYxFVVOR NFjpUnhKSzVyPUCuNlIh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ydmFOTE2VTx?= MnfsTWM2OD1yLkC0JO69VQ>? NEDwRlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H358 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHEUXNQ M4L5UmlEPTB;MD6xJO69VQ>? NYTuTGJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H460 M4LLUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXqUYpFVVOR MonnTWM2OD1yLkGzJO69VQ>? M3PVXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
CMK NHPSOFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETpXIZKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViV2SgTmFMKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xPzVizszN NG\vbGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO1NlEzPCd-MkWzOVIyOjR:L3G+
CMK M{juWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm4TY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOlNFKG23dHH0bY9vKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yPjNizszN Mo[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK NUft[YU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrrTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOVczXiCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25? M{XQNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
HT93A M2D3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHyzfmE{OjBibl2= MVS1JIQ> NGjQRYxFVVOR NFLDNJZKdmirYnn0bY9vKG:oIFfDV{1HKGmwZIXj[YQh\3KjboXsc4N6fGmlIHTp[oZmemWwdHnheIlwdg>? NFvJdog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwOVk3Oid-MkW4NFU6PjJ:L3G+
SET-2 MWjDfZRwfG:6aXOgRZN{[Xl? NH;STXo2KM7:TR?= NVmyVVBZPDhiaB?= NULDOmptS3m2b4TvfIlkKGmwZHX4QVE5Njdn MnriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{GzOFkoRjJ3OUOxN|Q6RC:jPh?=
HEL MVzDfZRwfG:6aXOgRZN{[Xl? M2mxO|Uh|ryP NX3aOZdXPDhiaB?= MmrsR5l1d3SxeHnjJIlv\GW6PUGyMlIm MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl|MUO0PUc,OjV7M{GzOFk9N2F-
Human monocyte M1rnbWtqdmG|ZTDBd5NigQ>? NYrHOHhtUW6qaXLpeIlwdiCxZjDKRWszNzFiaX6gbJVu[W5ibX;uc4N6fGW|IHX4dJJme3OrbnegR2QyPCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmITnfhcY1iNXO2aX31cIF1\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCzNe69VQ>? NIS2SFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
Human monocyte NGrNVoxMcW6jc3WgRZN{[Xl? MmjuTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJI1wdm:leYTld{BmgHC{ZYPzbY5oKEOGMUSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0Zvc4TpcZVt[XSnZDDTWGFVPWFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAzPs7:TR?= MnH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human T cell MmHTT4lv[XOnIFHzd4F6 NFe5S4hKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 MWTLbY5ie2ViQYPzZZk> M4q0TVIxKG2rbh?= NIT6O4tFVVOR NIPQU5NKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
TF1 NXXMZ|lDU2mwYYPlJGF{e2G7 M{fBblIxKG2rbh?= MmLtSG1UVw>? NHL6e3hKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVCRLXnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxNu69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
Sf9 cells MnfsTmFMKGmwaHnibZRqd25iYYPzZZk> NWi0NJJIOSCq MonPT4khRSByLkCwNFEh|ryP NFfRO5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2PFQ5PCd-MkO2Olg1QDR:L3G+
Sf9 cells NHvES5dLSUtiaX7obYJqfGmxbjDhd5NigQ>? M2LONlEhcA>? NU\XVJdqU2liPTCwMlAxODJizszN NV3ZV2hZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf9 cells Mn3HTmFMKGmwaHnibZRqd25iYYPzZZk> Ml3YNUBp MYDLbUA:KDBwMECwOUDPxE1? NEjOPHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2PFQ5PCd-MkO2Olg1QDR:L3G+
SET2 cells MWXKRWshcW6qaXLpeIlwdiCjc4PhfS=> MYLJR|UxKD1iMD6wNFE5PCEQvF2= NX;MPVlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOlE3PjBpPkKzNFYyPjZyPD;hQi=>
Sf21 cells MX\KRWshcW6qaXLpeIlwdiCjc4PhfS=> NFXIfFIyKGh? M1LmW2lEPTBiPTCwMlAxOjhizszN MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
Sf21 cells Mn34TmFMKGmwaHnibZRqd25iYYPzZZk> NIrwOlA3OCCvaX6= M1f5cGlEPTBiPTCwMlAxOyEQvF2= M121TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUO3N|U6Lz5{N{GzO|M2QTxxYU6=
Sf9 cells NXfVb4JyUkGNIHnubIljcXSrb36gZZN{[Xl? NGHCfW4yKGh? NHW4N|ZMcSB;IECuNFA{OiEQvF2= NIC0Opk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2PFQ5PCd-MkO2Olg1QDR:L3G+
Sf21 cells MV;KRWshcW6qaXLpeIlwdiCjc4PhfS=> NUjVTFhMOSCq MXLJR|UxKD1iMD6wNFM{KM7:TR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
TF1 cells NV3jRmVIUkGNIHnubIljcXSrb36gZZN{[Xl? NVXEfZRXOzBibXnu NGX6dnlKSzVyIE2gNE4xODZ6NTFOwG0> MnLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkG2OlAoRjJ|ME[xOlYxRC:jPh?=
CD34+ cells M2W5fmpCUyCrbnjpZol1cW:wIHHzd4F6 NIj5UoRKSzVyIE2gNE4xODhizszN NFSyOIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyO|QzOyd-Mk[5Nlc1OjN:L3G+
TF1 cells NWfvSZplUkGNIHnubIljcXSrb36gZZN{[Xl? Mnu3NlAhdWmw NXjvUXZxTUN3MDC9JFAvODF{IN88US=> NGrRcZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
Sf21 cells MUDUXWszKGmwaHnibZRqd25iYYPzZZk> NVO5fmlMOSCq MV7JR|UxKD1iMD6wNVkh|ryP M1nXUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUmxOFAzLz5{MkW5NVQxOjxxYU6=
T cells NETFNJBLSUtiaX7obYJqfGmxbjDhd5NigQ>? NXK1Z|I3UUN3MDC9JFAvODJ|IN88US=> NGrufYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
T cells NFuybVZLSUtiaX7obYJqfGmxbjDhd5NigQ>? NIHsbZBKSzVyIE2gNE4xOjNizszN MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 cells M2LybmpCUyCrbnjpZol1cW:wIHHzd4F6 NIXNToMzOCCvaX6= MkTZSWM2OCB;IECuNFI1KM7:TR?= NGHHNVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
T cells NFvQbIJLSUtiaX7obYJqfGmxbjDhd5NigQ>? M1jNW2lEPTBiPTCwMlA{OSEQvF2= M4HNN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells MoLyTmFMKGmwaHnibZRqd25iYYPzZZk> NH;ERYhKSzVyIE2gNE4xOzFizszN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
PBMC cells NFTHTZVLSUtiaX7obYJqfGmxbjDhd5NigQ>? NFzySYRKSzVyIE2gNE4xPCEQvF2= MnXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
Sf21 cells MWXKRWshcW6qaXLpeIlwdiCjc4PhfS=> MkTENUBp NHr5VYRKSzVyIE2gNE41OjhizszN MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
PBMC cells MVfTWGFVPSCrbnjpZol1cW:wIHHzd4F6 NIDV[nlKSzVyIE2gNE41PDhizszN MlPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
CD34+ cells MlzITmFMKGmwaHnibZRqd25iYYPzZZk> M3LJfVQ2KG2rbh?= M1;jcmlEPTBiPTCwMlY4PyEQvF2= M3:xblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVM{Lz5{NESxO|U{OzxxYU6=

... 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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 SDS / 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 SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04908735 Recruiting Drug: Ruxolitinib Hematopoietic Stem Cell Transplant (HSCT)|Bronchiolitis Obliterans (BO) Children''s Hospital Medical Center Cincinnati September 2021 Phase 2
NCT04551131 Recruiting Drug: Ruxolitinib|Drug: Dexamethasone|Drug: Etoposide Hemophagocytic Lymphohistiocytosis St. Jude Children''s Research Hospital|Incyte Corporation|North American Consortium for Histiocytosis July 13 2021 Phase 1|Phase 2
NCT04543279 Recruiting Drug: Fostamatinib|Drug: Ruxolitinib Myelofibrosis Washington University School of Medicine|Rigel Pharmaceuticals May 3 2021 Phase 2
NCT04480086 Active not recruiting Drug: Mivebresib|Drug: Navitoclax|Drug: Ruxolitinib Myelofibrosis (MF) AbbVie March 17 2021 Phase 1
NCT04485260 Recruiting Drug: KRT-232|Drug: Ruxolitinib Myelofibrosis Kartos Therapeutics Inc. January 28 2021 Phase 1|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

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