Ruxolitinib (INCB018424)

For research use only.

Catalog No.S1378

390 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 390 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 MUjGeY5kfGmxbjDBd5NigQ>? MXm1NEDPxE1? M3f0[lI1KGh? NUXmO2NmTE2VTx?= M4Xm[GlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NULmWotXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU182 M1WyOWZ2dmO2aX;uJGF{e2G7 NXfPfo1lPTBizszN M2OxfVI1KGh? M4\NOWROW09? NGrIbmFKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NGXQfIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 NW\LO3hiTnWwY4Tpc44hSXO|YYm= MlvrOVAh|ryP MXmyOEBp NYTWNXc4TE2VTx?= M4jCTmlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NVzTfZlpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU423 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe1NEDPxE1? NFXKW2s1QCCq M17U[mROW09? MkfGQlgyLSC{ZXT1Z5Rqd25? M36yVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 NF7XPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v5VFUxKM7:TR?= NYW3cm8{PDhiaB?= NHPkeJdFVVOR NE[4XmE,PjRnIILl[JVkfGmxbh?= M1LjSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
HuH7 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUO1NEDPxE1? NH7oXVI1QCCq NFu4OmpFVVOR M{nVdF45OiVicnXkeYN1cW:w M4DHSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
RKO MmfzRZBweHSxc3nzJGF{e2G7 MUGyOUDPxE1? MnmwOFghcA>? MnjYSG1UVw>? NH2yZmdKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 MY\BdI9xfG:|aYOgRZN{[Xl? NEfJ[4IzPSEQvF2= M{\ye|Q5KGh? MmTsSG1UVw>? MlTETY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? NWnESplURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
DLD-1 M3LGRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnqSYpyPTBizszN NHiyR5c1QCCq M1:1[WROW09? NFrVS5FKSzVyPUG1MlUyKM7:TR?= M2DmVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO Ml3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfWW2xOPTBizszN MX60PEBp MlTzSG1UVw>? NFrmT2tKSzVyPUG0Mlc3KM7:TR?= NXGybpdURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO NGPZSWJMcW6jc3WgRZN{[Xl? NHO2PG0zPSEQvF2= MnzqOFghcA>? MYfEUXNQ M2TxXIRw\XNibn;0JIlvcGmkaYSgTmFMOSCyaH;zdIhwenmuYYTpc44> NFLXPVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 NIi3SpBMcW6jc3WgRZN{[Xl? NEfSRmUzPSEQvF2= MmnzOFghcA>? NYe4RmVDTE2VTx?= MUnJcohq[mm2aX;uJI9nKEqDS{KgdIhwe3Cqb4L5cIF1cW:w NGq4PHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
RKO M3;GeWtqdmG|ZTDBd5NigQ>? NHrPd3AzPSEQvF2= M1rTSFQ5KGh? NXPRfZd6TE2VTx?= NXz1b5liUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MnzNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 M3HBUmtqdmG|ZTDBd5NigQ>? NYLSeGZpOjVizszN Moj3OFghcA>? NX7lWm0yTE2VTx?= MXrJcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w NV7TOoxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
BaF3 M{jv[2tqdmG|ZTDBd5NigQ>? NVfoU3J[QDBibl2= NH7oTHA3KGh? NITlPGZFVVOR M3fuTXJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\sLiU2TBWFUhcW5iSlHLNnY3OTeILX31eIF1\WRiQlHGN{1GWE:UIHPlcIw> MmfuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{M{e3PVEoRjJ2MkO3O|kyRC:jPh?=
Huh7 NFnhdZFHfW6ldHnvckBCe3OjeR?= NHnoZYsyKM7:TR?= MmHCNVYhcA>? M1L5dmROW09? NUfUU2V{UW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
HepG2 M3Xrb2Z2dmO2aX;uJGF{e2G7 NGnBcI8yKM7:TR?= NVzMcWpnOTZiaB?= NVfwcnF{TE2VTx?= NVf6T2NbUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? NHvmR2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
Hep3B NHu5ZYNHfW6ldHnvckBCe3OjeR?= NXK4WWdDOSEQvF2= NXnvU2szOTZiaB?= M1;OR2ROW09? MUHJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8h[WO2aY\lJHNVSVR|IIfpeIghUUN3MDDv[kB,PTBizszN NEXISY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
NCI-H2347 MoTFRZBweHSxc3nzJGF{e2G7 NFfydVE{OCCwTR?= M1\LZ|Q5KGh? MkC4SG1UVw>? M3m4bmlv\HWldHnvckBw\iCjcH;weI9{cXN? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 MYLBdI9xfG:|aYOgRZN{[Xl? NH\obJo{OCCwTR?= NGrIV5E1QCCq M2\YcWROW09? M1\kbmlv\HWldHnvckBw\iCjcH;weI9{cXN? NGTnUXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP NWLHV|c4SXCxcITvd4l{KEG|c3H5 M37R[lMxKG6P NF3rdFc1QCCq NYDJWJRSTE2VTx?= MlPETY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MkLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H1299 MkXDSpVv[3Srb36gRZN{[Xl? NEP2UYI{OCCwTR?= NWLWNFdjPDhiaB?= MXHEUXNQ MnnLSI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? M4\TSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 MnvmSpVv[3Srb36gRZN{[Xl? MX[zNEBvVQ>? NXLZcJpMPDhiaB?= MljjSG1UVw>? MVHE[YNz\WG|ZTDpckBD[2x{IHX4dJJme3Orb36= NIqyXVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP MVXGeY5kfGmxbjDBd5NigQ>? M17POFMxKG6P NGnIUVY1QCCq MWPEUXNQ MUTEc5dvNXKnZ4XsZZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9v M1PtfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 M2PwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrWPXEzTE2VTx?= NYPPNVRXUUN3ME2wMlE4KM7:TR?= NG\obYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 NF7u[pBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIH4SJZFVVOR MVnJR|UxRTBwMkig{txO NIGySlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP NUfuWmJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHEUXNQ MlXFTWM2OD1yLkKyJO69VQ>? NGTpUos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549 Mk\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLMeFdFVVOR NEXCPXpKSzVyPUCuNFQh|ryP M2fHZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H358 MoDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mln4SG1UVw>? MWDJR|UxRTBwMTFOwG0> MkXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H460 NGHnPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzEUXNQ NFzRe2RKSzVyPUCuNVMh|ryP MlzEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
CMK NWrsfYtxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHVTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKFeWIFrBT{Bk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFc2KM7:TR?= MlHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK NXnSS|JFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G2N2QhdXW2YYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlE3OyEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MkGyOEc,OjV|NUKxNlQ9N2F-
CMK NGPtO|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjKUpJ4UW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPTd{VjDteZRifGmxbjDj[YxtKHC{b3zp[oVz[XSrb36= NVrjUHpbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
HT93A MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HHOFMzOCCwTR?= M1nENFUh\A>? NXfNVm9OTE2VTx?= MXfJcohq[mm2aX;uJI9nKEeFUz3GJIlv\HWlZXSg[5JidnWub3P5eIlkKGSrZn\ldoVvfGmjdHnvci=> NFe3NI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwOVk3Oid-MkW4NFU6PjJ:L3G+
SET-2 NELIbpdEgXSxdH;4bYMhSXO|YYm= NEDpUYQ2KM7:TR?= M4fGVFQ5KGh? MXLDfZRwfG:6aXOgbY5l\Xh;MUiuO{U> NWj2bVlURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|E{PDlpPkK1PVMyOzR7PD;hQi=>
HEL MWPDfZRwfG:6aXOgRZN{[Xl? NGD5[HQ2KM7:TR?= MWm0PEBp MYDDfZRwfG:6aXOgbY5l\Xh;MUKuNkU> M4L1UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
Human monocyte NX\r[pJDU2mwYYPlJGF{e2G7 MXnJcohq[mm2aX;uJI9nKEqDS{KvNUBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWZP\2GvbXGtd5RqdXWuYYTl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODNzzszN Mkf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human monocyte NIXMcFJMcW6jc3WgRZN{[Xl? MY\Jcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI3|ryP NYPhdHdxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
Human T cell NF35SWxMcW6jc3WgRZN{[Xl? M3P6TmlvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyN:69VQ>? NX3ibo4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
TF1 M2HjWGtqdmG|ZTDBd5NigQ>? NGrDSlczOCCvaX6= NX72OYVlTE2VTx?= M2\GO2lvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEK0{txO MorHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
TF1 MWTLbY5ie2ViQYPzZZk> NYnlZVhEOjBibXnu MV3EUXNQ MV;Jcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVEWgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzMt88US=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
Sf9 cells NV:xNJFRUkGNIHnubIljcXSrb36gZZN{[Xl? NGHoZVMyKGh? NVO1dXozU2liPTCwMlAxODFizszN NW\nUIhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf9 cells M{K3XmpCUyCrbnjpZol1cW:wIHHzd4F6 MWKxJIg> M2D2XGtqKD1iMD6wNFAzKM7:TR?= MnfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4Nki0PFQoRjJ|Nk[4OFg1RC:jPh?=
Sf9 cells MkH4TmFMKGmwaHnibZRqd25iYYPzZZk> MlX0NUBp NYjZfldSU2liPTCwMlAxODVizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
SET2 cells MYPKRWshcW6qaXLpeIlwdiCjc4PhfS=> MnTzTWM2OCB;IECuNFAyQDRizszN NUXVPHI5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOlE3PjBpPkKzNFYyPjZyPD;hQi=>
Sf21 cells MljsTmFMKGmwaHnibZRqd25iYYPzZZk> M4HnWFEhcA>? MWHJR|UxKD1iMD6wNFI5KM7:TR?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
Sf21 cells NXmweYVPUkGNIHnubIljcXSrb36gZZN{[Xl? MWq2NEBucW5? NGPLPFFKSzVyIE2gNE4xODNizszN MoXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{ezOVkoRjJ5MUO3N|U6RC:jPh?=
Sf9 cells MX\KRWshcW6qaXLpeIlwdiCjc4PhfS=> M4rY[FEhcA>? MmLBT4khRSByLkCwN|Ih|ryP NYG5O3BGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf21 cells MY\KRWshcW6qaXLpeIlwdiCjc4PhfS=> MWixJIg> NHzFPHVKSzVyIE2gNE4xODN|IN88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
TF1 cells MkfkTmFMKGmwaHnibZRqd25iYYPzZZk> NVLw[491OzBibXnu M2PSfWlEPTBiPTCwMlAxPjh3IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB4MU[2NEc,OjNyNkG2OlA9N2F-
CD34+ cells MnPFTmFMKGmwaHnibZRqd25iYYPzZZk> NF3aR|VKSzVyIE2gNE4xODhizszN NUHZPHdSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5Nlc1OjNpPkK2PVI4PDJ|PD;hQi=>
TF1 cells NX21eJh5UkGNIHnubIljcXSrb36gZZN{[Xl? NWrrUoRROjBibXnu NXzjfIs2TUN3MDC9JFAvODF{IN88US=> M2jNUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nkm4NFg1Lz5{Mk[5PFA5PDxxYU6=
Sf21 cells M3nPcHR[UzJiaX7obYJqfGmxbjDhd5NigQ>? MWKxJIg> NGfVXlFKSzVyIE2gNE4xOTlizszN NUXKdGdXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVE1ODJpPkKyOVkyPDB{PD;hQi=>
T cells NH7BR3ZLSUtiaX7obYJqfGmxbjDhd5NigQ>? MUDJR|UxKD1iMD6wNlMh|ryP Ml;HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
T cells NIXEeVVLSUtiaX7obYJqfGmxbjDhd5NigQ>? MlHaTWM2OCB;IECuNFI{KM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 cells M2XKSWpCUyCrbnjpZol1cW:wIHHzd4F6 M2HQOFIxKG2rbh?= MX\FR|UxKD1iMD6wNlQh|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
T cells M1zSW2pCUyCrbnjpZol1cW:wIHHzd4F6 M1zWNWlEPTBiPTCwMlA{OSEQvF2= M2rGPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells NH\4Z|NLSUtiaX7obYJqfGmxbjDhd5NigQ>? NFyyc3BKSzVyIE2gNE4xOzFizszN M2DmflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
PBMC cells Mmf0TmFMKGmwaHnibZRqd25iYYPzZZk> NInXbmlKSzVyIE2gNE4xPCEQvF2= NXHQSHFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5Nlc1OjNpPkK2PVI4PDJ|PD;hQi=>
Sf21 cells MYDKRWshcW6qaXLpeIlwdiCjc4PhfS=> MlHkNUBp NVjOfZpRUUN3MDC9JFAvPDJ6IN88US=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
PBMC cells NXS5U4t{W1SDVEWgbY5pcWKrdHnvckBie3OjeR?= M336dWlEPTBiPTCwMlQ1QCEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{N{SyN{c,OjZ7Mke0NlM9N2F-
CD34+ cells MnzZTmFMKGmwaHnibZRqd25iYYPzZZk> Ml7oOFUhdWmw MXLJR|UxKD1iMD62O|ch|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{WzN{c,OjR2MUe1N|M9N2F-

... 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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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04543279 Recruiting Drug: Fostamatinib|Drug: Ruxolitinib Myelofibrosis Washington University School of Medicine|Rigel Pharmaceuticals May 3 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 March 8 2021 Phase 1|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
NCT04359290 Active not recruiting Drug: Ruxolitinib administration ARDS Human|COVID Philipps University Marburg Medical Center July 1 2020 Phase 2
NCT04414098 Not yet recruiting Drug: INC424 / Ruxolitinib COVID-19 Marcelo Iastrebner|Novartis|Clinica Zabala June 1 2020 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