Ruxolitinib (INCB018424)

For research use only.

Catalog No.S1378

375 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 375 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 NXXrRY1YTnWwY4Tpc44hSXO|YYm= NUnXWGlQPTBizszN NI\rWGMzPCCq MXjEUXNQ NFOwd4xKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NHrNZos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 NFvzNm5HfW6ldHnvckBCe3OjeR?= MYC1NEDPxE1? NF;ke5czPCCq NG[2U3pFVVOR MWDJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NWrVO3pzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
HuH7 MWPGeY5kfGmxbjDBd5NigQ>? NX\6S2syPTBizszN NVT6RVRuOjRiaB?= Mn\pSG1UVw>? M{jINGlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 NELtd|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU423 NVnnRo9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV61NEDPxE1? NFP5V4Y1QCCq M1nTXGROW09? MWW+PFEmKHKnZIXjeIlwdg>? NWTtXGxQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU182 NEjLeo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLzOVAh|ryP NVfnd3h7PDhiaB?= NWjZRVllTE2VTx?= NXXCZ5BVRjZ2JTDy[YR2[3Srb36= NEDUW4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 M4XsWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYW1NEDPxE1? MVy0PEBp NV;PSoZpTE2VTx?= NXvzfZlFRjh{JTDy[YR2[3Srb36= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
RKO MkDTRZBweHSxc3nzJGF{e2G7 Mn7yNlUh|ryP NELnZ|k1QCCq MXjEUXNQ NU\ERWRnUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= M2\QOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 NH3leWhCeG:ydH;zbZMhSXO|YYm= NWXXRm9yOjVizszN NIPrUo01QCCq MU\EUXNQ MnXYTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? NIqyTFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 NGTvToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfwV2FZPTBizszN NF\Vd5k1QCCq MW\EUXNQ NHmxWVVKSzVyPUG1MlUyKM7:TR?= M1nGSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO NGnGTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHFOVAh|ryP NV;EZ21pPDhiaB?= MYnEUXNQ M2foW2lEPTB;MUSuO|Yh|ryP NIHaWZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
RKO Ml3jT4lv[XOnIFHzd4F6 MWWyOUDPxE1? NHHhcpA1QCCq NH[xN2dFVVOR M4H5[oRw\XNibn;0JIlvcGmkaYSgTmFMOSCyaH;zdIhwenmuYYTpc44> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NVvoNYhYU2mwYYPlJGF{e2G7 M4O1fVI2KM7:TR?= MXO0PEBp MYXEUXNQ M4GzNWlvcGmkaYTpc44hd2ZiSlHLNkBxcG:|cHjvdplt[XSrb36= M4XCPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MkPiT4lv[XOnIFHzd4F6 NUK5WXJWOjVizszN M4nLOVQ5KGh? Mm\hSG1UVw>? NXS1PHA2UW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> Mln6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 M{fq[GtqdmG|ZTDBd5NigQ>? M4jybFI2KM7:TR?= MUO0PEBp MUfEUXNQ M1H1bmlvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36= NV7TOmd2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
BaF3 Mo\lT4lv[XOnIFHzd4F6 NFPpNZM5OCCwTR?= MU[2JIg> MmW5SG1UVw>? NHHvem5T\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2cEoGPURXQ2KGmwIFrBT|JXPjF5Rj3teZRifGWmIFLBSlMuTVCRUjDj[Yxt MmfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{M{e3PVEoRjJ2MkO3O|kyRC:jPh?=
Huh7 MoTTSpVv[3Srb36gRZN{[Xl? NFnkfogyKM7:TR?= MnP0NVYhcA>? NVXWW29xTE2VTx?= MVTJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz NEfWTnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
HepG2 MXPGeY5kfGmxbjDBd5NigQ>? NWH3SmxwOSEQvF2= NEG0dnUyPiCq MnOxSG1UVw>? MYrJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz NXLMXYtFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFE3QDlpPkK0OVAyPjh7PD;hQi=>
Hep3B MlHOSpVv[3Srb36gRZN{[Xl? NH7Ed3QyKM7:TR?= NXOxWHdkOTZiaB?= M372NmROW09? MYDJcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8h[WO2aY\lJHNVSVR|IIfpeIghUUN3MDDv[kB,PTBizszN NIfnZVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
NCI-H2347 MV\BdI9xfG:|aYOgRZN{[Xl? MYmzNEBvVQ>? NUHWWXlCPDhiaB?= NIHCTJpFVVOR M3vsUWlv\HWldHnvckBw\iCjcH;weI9{cXN? NHvuPIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 NEPDR3lCeG:ydH;zbZMhSXO|YYm= NXPWTndyOzBibl2= M3znVlQ5KGh? M2Kw[GROW09? MlH0TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NVTGbZdsSXCxcITvd4l{KEG|c3H5 NYHj[401OzBibl2= NGTMbZg1QCCq NGPxbZNFVVOR NYfVR3FQUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M{ftUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 MkX1SpVv[3Srb36gRZN{[Xl? NX\sb21HOzBibl2= M4PCe|Q5KGh? M4i4emROW09? MmnZSI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? M1\kc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 MYTGeY5kfGmxbjDBd5NigQ>? M4r1bVMxKG6P NGDRVYg1QCCq NGTs[HJFVVOR Mn31SIVkemWjc3WgbY4hSmOuMjDlfJBz\XO|aX;u M2i3e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP NITFTI1HfW6ldHnvckBCe3OjeR?= NYTWT5V1OzBibl2= Mk\nOFghcA>? MmK0SG1UVw>? M2PKZWRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? NFnKZY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H2347 NYjoVJZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXBR21FVVOR MUHJR|UxRTBwMUeg{txO M4KySFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 M2\aVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\Pb3BFVVOR MXzJR|UxRTBwMkig{txO NUPPeG4zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP Mnf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;4SG1UVw>? Mn65TWM2OD1yLkKyJO69VQ>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549 NH70cnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3jclFvTE2VTx?= MV3JR|UxRTBwMESg{txO Mom4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H358 M4D3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnEUXNQ NYiwOI1VUUN3ME2wMlEh|ryP M2nhTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H460 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzEUXNQ MV7JR|UxRTBwMUOg{txO Ml:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
CMK MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHtfVZxUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=> NH\qSIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO1NlEzPCd-MkWzOVIyOjR:L3G+
CMK NFTpVJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3noTWlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVY{TCCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTZ|IN88US=> MkjyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK NIjSPYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4K4fWlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVU4OlZibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:w MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MkGyOEc,OjV|NUKxNlQ9N2F-
HT93A NUH3UnRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LmOlMzOCCwTR?= M2\aUVUh\A>? NHrrUZVFVVOR M4nJZWlvcGmkaYTpc44hd2ZiR1PTMWYhcW6mdXPl[EBoemGwdXzvZ5l1cWNiZHnm[oVz\W62aXH0bY9v M2ezTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEC1PVYzLz5{NUiwOVk3OjxxYU6=
SET-2 MlHER5l1d3SxeHnjJGF{e2G7 NIq2bY02KM7:TR?= NF3nN|M1QCCq Mn;ZR5l1d3SxeHnjJIlv\GW6PUG4Mlcm MkD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{GzOFkoRjJ3OUOxN|Q6RC:jPh?=
HEL MUjDfZRwfG:6aXOgRZN{[Xl? MofSOUDPxE1? MXu0PEBp NEfVd45EgXSxdH;4bYMhcW6mZYi9NVIvOiV? NWDNZ2R4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|E{PDlpPkK1PVMyOzR7PD;hQi=>
Human monocyte Mo\ET4lv[XOnIFHzd4F6 M{ftZWlvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> M3\MWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
Human monocyte NX3ESJBqU2mwYYPlJGF{e2G7 NGjVeZVKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGdONUOVRj3zeIlufWyjdHXkJHNVSVR3YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODJ4zszN MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
Human T cell M2fjRmtqdmG|ZTDBd5NigQ>? M{XmWmlvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyN:69VQ>? NEPkVWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
TF1 MVrLbY5ie2ViQYPzZZk> M{XYUVIxKG2rbh?= NIL6fWVFVVOR NFz5UYVKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
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Sf9 cells MnezTmFMKGmwaHnibZRqd25iYYPzZZk> MVGxJIg> NXK1U5p4U2liPTCwMlAxOzJizszN M3HVe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf21 cells M{\kdWpCUyCrbnjpZol1cW:wIHHzd4F6 NGXVVXMyKGh? NVzXe2JkUUN3MDC9JFAvODB|MzFOwG0> NVe1eFNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVE1ODJpPkKyOVkyPDB{PD;hQi=>
TF1 cells M4DjZ2pCUyCrbnjpZol1cW:wIHHzd4F6 M4PIZ|MxKG2rbh?= NYrSVW9qUUN3MDC9JFAvODB4OEWg{txO NUnZNoJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOlE3PjBpPkKzNFYyPjZyPD;hQi=>
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T cells MnrCTmFMKGmwaHnibZRqd25iYYPzZZk> M1y4XmlEPTBiPTCwMlA{OSEQvF2= M1f3SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
PBMC cells NWHHN3NKUkGNIHnubIljcXSrb36gZZN{[Xl? M33BcWlEPTBiPTCwMlA1KM7:TR?= M{\QWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
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PBMC cells MYPTWGFVPSCrbnjpZol1cW:wIHHzd4F6 NX7z[29zUUN3MDC9JFAvPDR6IN88US=> M1PCXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
CD34+ cells M4ryempCUyCrbnjpZol1cW:wIHHzd4F6 NIDYSIE1PSCvaX6= MYHJR|UxKD1iMD62O|ch|ryP MkHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1N|MoRjJ2NEG3OVM{RC:jPh?=

... 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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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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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:

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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