Ruxolitinib (INCB018424)

Catalog No.S1378

For research use only.

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.

Ruxolitinib (INCB018424) Chemical Structure

CAS No. 941678-49-5

Selleck's Ruxolitinib (INCB018424) has been cited by 437 publications

Purity & Quality Control

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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 MVXGeY5kfGmxbjDBd5NigQ>? MnnzOVAh|ryP M1rHXFI1KGh? NFTEeYFFVVOR MVTJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? NFKyUGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 Ml;GSpVv[3Srb36gRZN{[Xl? M1jTOVUxKM7:TR?= MWmyOEBp MYrEUXNQ MWHJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
HuH7 MV7GeY5kfGmxbjDBd5NigQ>? NX7SZmNjPTBizszN MoS0NlQhcA>? MmHQSG1UVw>? Mk\RTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NWHTUpNWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU423 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfRT2Y2OCEQvF2= NXToWI5pPDhiaB?= M1rOVmROW09? NYLQTIE{RjhzJTDy[YR2[3Srb36= M3iwN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61NEDPxE1? NH\acI01QCCq M2n1Z2ROW09? MojIQlY1LSC{ZXT1Z5Rqd25? NFS2NpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 NUDpfVZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXywepRRPTBizszN M{m0UVQ5KGh? MX\EUXNQ MVm+PFImKHKnZIXjeIlwdg>? MkS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
RKO NFvPVY1CeG:ydH;zbZMhSXO|YYm= NHTvSYwzPSEQvF2= NVLvdWlTPDhiaB?= M1fIbWROW09? M1T2Smlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 MnzoRZBweHSxc3nzJGF{e2G7 MYSyOUDPxE1? M1yx[lQ5KGh? Mo\WSG1UVw>? NGO2R25KdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= NEjaXFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmeyOVAh|ryP NUC2Omo{PDhiaB?= NHTad3JFVVOR M3;LWWlEPTB;MUWuOVEh|ryP NVrsOW5GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO NFzaOnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16wclUxKM7:TR?= NUDLemd{PDhiaB?= Mn;lSG1UVw>? Mnq1TWM2OD1zND63OkDPxE1? MmDPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
RKO MXTLbY5ie2ViQYPzZZk> M1XJcFI2KM7:TR?= MUi0PEBp NYLGXoJKTE2VTx?= MkfX[I9meyCwb4SgbY5pcWKrdDDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MmrwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 MljuT4lv[XOnIFHzd4F6 NUniXolxOjVizszN MlTMOFghcA>? M2LSWGROW09? M3GwNmlvcGmkaYTpc44hd2ZiSlHLNkBxcG:|cHjvdplt[XSrb36= M{HN[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MX\LbY5ie2ViQYPzZZk> M1j0RVI2KM7:TR?= NGHDN201QCCq NF;rPVdFVVOR NU\JSmhpUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> NGH3Rmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 MVPLbY5ie2ViQYPzZZk> MYWyOUDPxE1? MkjTOFghcA>? MYrEUXNQ Mn;ETY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= NFjyfHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
BaF3 NY\Hc5o5U2mwYYPlJGF{e2G7 MoW4PFAhdk1? Mk\GOkBp MV\EUXNQ M4DZcHJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\sLiU2TBWFUhcW5iSlHLNnY3OTeILX31eIF1\WRiQlHGN{1GWE:UIHPlcIw> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ|N{e5NUc,OjR{M{e3PVE9N2F-
Huh7 MoDMSpVv[3Srb36gRZN{[Xl? NVfrSWpkOSEQvF2= MVqxOkBp Mmi5SG1UVw>? M{DPcGlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> M2\leFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
HepG2 NUTYd3lyTnWwY4Tpc44hSXO|YYm= NGrheGEyKM7:TR?= MnzjNVYhcA>? NFf0N|lFVVOR NXLpOWxSUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
Hep3B MVHGeY5kfGmxbjDBd5NigQ>? NETzT5kyKM7:TR?= NXzCUm1zOTZiaB?= NV;GZnBNTE2VTx?= NWX1UpRvUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIHHjeIl3\SCVVFHUN{B4cXSqIFnDOVAhd2ZifkWwJO69VQ>? MnPXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEG2PFkoRjJ2NUCxOlg6RC:jPh?=
NCI-H2347 NVjCPZg3SXCxcITvd4l{KEG|c3H5 M3XwOVMxKG6P M1LKfFQ5KGh? M3nhNmROW09? MXjJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NFvZcHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 NYXmTlhPSXCxcITvd4l{KEG|c3H5 MkDzN|Ahdk1? NUfOfW5vPDhiaB?= NIP5dYRFVVOR NVzDWnFoUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NUK4U4k4SXCxcITvd4l{KEG|c3H5 MXuzNEBvVQ>? MYK0PEBp MYHEUXNQ M37ON2lv\HWldHnvckBw\iCjcH;weI9{cXN? NH\ZUpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 M{P1PGZ2dmO2aX;uJGF{e2G7 M2nRVFMxKG6P NVLXZlVkPDhiaB?= MV7EUXNQ MkXlSI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H2347 MVfGeY5kfGmxbjDBd5NigQ>? NEHpUJI{OCCwTR?= M{HldFQ5KGh? MoDsSG1UVw>? MoLtSIVkemWjc3WgbY4hSmOuMjDlfJBz\XO|aX;u MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NXrZPWdnTnWwY4Tpc44hSXO|YYm= Mn;3N|Ahdk1? NWTLe|ZMPDhiaB?= MVjEUXNQ M{\LV2Rwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? MmnjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H2347 NX;M[4F7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLwTZVNTE2VTx?= M2C3OGlEPTB;MD6xO{DPxE1? M4rQZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 M{TPTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXPb2VpTE2VTx?= NEnSN4JKSzVyPUCuNlgh|ryP NVLIPVN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP M3[xXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULpVoxTTE2VTx?= NFv2[W5KSzVyPUCuNlIh|ryP MmLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
A549 M37XNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDEUXNQ MkjzTWM2OD1yLkC0JO69VQ>? MmnkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H358 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPEUXNQ M2LH[mlEPTB;MD6xJO69VQ>? NYDLRWRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H460 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnEUXNQ NVfTXIx7UUN3ME2wMlE{KM7:TR?= MlP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
CMK NWnNVHdYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7SeYRKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViV2SgTmFMKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xPzVizszN NY\4e|A6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
CMK NHrUZWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G2N2QhdXW2YYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlE3OyEQvF2= M2XKWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK NVfvdGU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmj3TY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOVczXiCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25? NIW3ZZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO1NlEzPCd-MkWzOVIyOjR:L3G+
HT93A MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TI[FMzOCCwTR?= MmLqOUBl M4nNWmROW09? NUnZTnhJUW6qaXLpeIlwdiCxZjDHR3MuTiCrbnT1Z4VlKGe{YX71cI9kgXSrYzDkbYZn\XKnboTpZZRqd25? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThyNUm2Nkc,OjV6MEW5OlI9N2F-
SET-2 NIq1fZNEgXSxdH;4bYMhSXO|YYm= NI\K[202KM7:TR?= MlnDOFghcA>? NUTuOXp{S3m2b4TvfIlkKGmwZHX4QVE5Njdn MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl|MUO0PUc,OjV7M{GzOFk9N2F-
HEL NYjyRoRvS3m2b4TvfIlkKEG|c3H5 NGDMV3U2KM7:TR?= M3Oz[FQ5KGh? NH;mVVhEgXSxdH;4bYMhcW6mZYi9NVIvOiV? MlrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{GzOFkoRjJ3OUOxN|Q6RC:jPh?=
Human monocyte M2fYWGtqdmG|ZTDBd5NigQ>? M1HjV2lvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
Human monocyte NVz2eG9HU2mwYYPlJGF{e2G7 M{fwSGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gS20uS1OILYP0bY12dGG2ZXSgV3RCXDWjIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xOjcQvF2= NUnWeVJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
Human T cell MkPxT4lv[XOnIFHzd4F6 NUTXVWJQUW6qaXLpeIlwdiCxZjDKRWs{NzFiaX6gbJVu[W5iVDDj[YxteyCneIDy[ZN{cW6pIFPEN{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI{|ryP MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 NYPQb3B[U2mwYYPlJGF{e2G7 MXuyNEBucW5? MoC0SG1UVw>? MmPWTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkVOwG0> NXLvfIY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PVgxQDRpPkKyOlk5ODh2PD;hQi=>
TF1 M2nUSWtqdmG|ZTDBd5NigQ>? M{TqN|IxKG2rbh?= MX7EUXNQ NVXicodLUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEWSTz3pcoR2[2WmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNVLPxE1? NITQbYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
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Sf9 cells MV7KRWshcW6qaXLpeIlwdiCjc4PhfS=> M2[2e|EhcA>? NGC1[GZMcSB;IECuNFAxPSEQvF2= NH\Wfm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2PFQ5PCd-MkO2Olg1QDR:L3G+
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Sf21 cells MVzKRWshcW6qaXLpeIlwdiCjc4PhfS=> MX6xJIg> MkDSTWM2OCB;IECuNFAzQCEQvF2= NE[3bVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
Sf21 cells M3ztfGpCUyCrbnjpZol1cW:wIHHzd4F6 MmW4OlAhdWmw NXTuWnl5UUN3MDC9JFAvODB|IN88US=> NWD1TJFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|c{PTlpPkK3NVM4OzV7PD;hQi=>
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Sf21 cells NETITJpLSUtiaX7obYJqfGmxbjDhd5NigQ>? MV2xJIg> MYrJR|UxKD1iMD6wNFM{KM7:TR?= NFrpRZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
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Assay
Methods Test Index PMID
Western blot cleaved PARP / cleaved caspase3 ; p-JAK2 / p-AKT / p-MAPK / Bcl-xl / MCL-1 ; c-Myc / c-Jun / Cyclin B / Cyclin D / Bcl-2 / HIF-1α ; p-STAT3 29849942 30930994
Growth inhibition assay Cell viability ; Cell apoptosis ; Cell proliferation 29849942 29515770
Immunofluorescence α-tubulin 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05034822 Recruiting Drug: Ruxolitinib cream Atopic Dermatitis|Open Label Incyte Corporation|Innovaderm Research December 16 2021 Phase 1
NCT04908735 Recruiting Drug: Ruxolitinib Hematopoietic Stem Cell Transplant (HSCT)|Bronchiolitis Obliterans (BO) Children''s Hospital Medical Center Cincinnati November 12 2021 Phase 2
NCT05121142 Recruiting Drug: Ruxolitinib Acute-graft-versus-host Disease|Chronic Graft-versus-host-disease Children''s Hospital Medical Center Cincinnati October 27 2021 Phase 1
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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