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 462 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 M3;jXmZ2dmO2aX;uJGF{e2G7 MWW1NEDPxE1? MYeyOEBp NHjJdpFFVVOR M3;6OWlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 M3u2V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 M2D6TGZ2dmO2aX;uJGF{e2G7 MV61NEDPxE1? NFLK[I0zPCCq NX7UUFRZTE2VTx?= NXjNbGxFUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NVz2doRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
HuH7 NE[3NHRHfW6ldHnvckBCe3OjeR?= NEH1TIs2OCEQvF2= MlXKNlQhcA>? NYDV[5lWTE2VTx?= MnXuTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
SNU423 NFr2[HdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\POVAh|ryP NX:0[mExPDhiaB?= MofVSG1UVw>? NXSxeVdkRjhzJTDy[YR2[3Srb36= NUn4Wm9KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU182 M3vVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnJWXQ2OCEQvF2= MX[0PEBp MYjEUXNQ M4nlfl43PCVicnXkeYN1cW:w MkLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
HuH7 NV3EXVl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojqOVAh|ryP Ml:xOFghcA>? NF[zWFJFVVOR NIfrfnc,QDJnIILl[JVkfGmxbh?= M4TLRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
RKO MXLBdI9xfG:|aYOgRZN{[Xl? M4fnbVI2KM7:TR?= NVvZe5BRPDhiaB?= MUHEUXNQ MYXJcoR2[2W|IHHwc5B1d3OrczDifUBi[3SrdnH0bY5oKGOjc4Dhd4UhOw>? M4LCd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 MnqzRZBweHSxc3nzJGF{e2G7 NXraT3ZwOjVizszN M3q2PFQ5KGh? Mn;kSG1UVw>? NFTsSnBKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= NXHwNoN[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
DLD-1 M{\YZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MniyOVAh|ryP NIHIO|g1QCCq M3nMSWROW09? NVvlZnZSUUN3ME2xOU42OSEQvF2= MnOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
RKO MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LmcFUxKM7:TR?= Mmr6OFghcA>? M4HiN2ROW09? NFjqe|ZKSzVyPUG0Mlc3KM7:TR?= NXvnO3hXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO M{XjbmtqdmG|ZTDBd5NigQ>? M4jOblI2KM7:TR?= NVzPc2ZXPDhiaB?= MUjEUXNQ MVjkc4V{KG6xdDDpcohq[mm2IFrBT|EheGixc4Doc5J6dGG2aX;u M2XONlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 M1TmO2tqdmG|ZTDBd5NigQ>? NX3OUYRDOjVizszN M2rEdVQ5KGh? M1P3ZmROW09? NFfMbG1KdmirYnn0bY9vKG:oIFrBT|IheGixc4Doc5J6dGG2aX;u MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
RKO MULLbY5ie2ViQYPzZZk> NHX1dpgzPSEQvF2= MkLHOFghcA>? Mnv5SG1UVw>? M3T5OmlvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36= NHfLTWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 MoDzT4lv[XOnIFHzd4F6 NVrZdY5mOjVizszN Mm\YOFghcA>? NFrzWnVFVVOR Mn:zTY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= M3HDRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
BaF3 M2qwdmtqdmG|ZTDBd5NigQ>? NGTtfmo5OCCwTR?= NXPuUFRvPiCq M4m2c2ROW09? MlzaVoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nyqCVVFHUOUBqdiCMQVuyWlYyP0ZvbYX0ZZRm\CCEQV[zMWVRV1JiY3XscC=> NEjISZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|c6OSd-MkSyN|c4QTF:L3G+
Huh7 NFT4dnJHfW6ldHnvckBCe3OjeR?= MkK3NUDPxE1? MYixOkBp M2LCXGROW09? NH;adY5KdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9ic3nncoFtKHSxIGPURXQ{ M1;RblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
HepG2 MV;GeY5kfGmxbjDBd5NigQ>? MnTZNUDPxE1? MX6xOkBp MknXSG1UVw>? NYixcpJRUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? NYLDTGxmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1NFE3QDlpPkK0OVAyPjh7PD;hQi=>
Hep3B M3vtdWZ2dmO2aX;uJGF{e2G7 MVWxJO69VQ>? NW\4VXBKOTZiaB?= NFrpN|ZFVVOR MkniTY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKGGldHn2[UBUXEGWMzD3bZRpKEmFNUCgc4YhhjVyIN88US=> NI\hVXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
NCI-H2347 MmHQRZBweHSxc3nzJGF{e2G7 MX2zNEBvVQ>? M{H6U|Q5KGh? Moq0SG1UVw>? NYfWTZJZUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 Mkm5RZBweHSxc3nzJGF{e2G7 M3nlflMxKG6P NUfHSVBnPDhiaB?= MkW4SG1UVw>? MV;JcoR2[3Srb36gc4Yh[XCxcITvd4l{ NUXXcpNMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP M3;jU2Fxd3C2b4Ppd{BCe3OjeR?= MW[zNEBvVQ>? MmnZOFghcA>? M1;SbWROW09? NEn1OnVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 NF;rR5NHfW6ldHnvckBCe3OjeR?= MVmzNEBvVQ>? NGDDOHY1QCCq MkTkSG1UVw>? M2WwWmRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? MkTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H2347 M2fZS2Z2dmO2aX;uJGF{e2G7 M3\ZVlMxKG6P MYW0PEBp MXHEUXNQ M3TrO2Rm[3KnYYPlJIlvKEKlbEKg[ZhxemW|c3nvci=> M2T3XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP NIjYU|RHfW6ldHnvckBCe3OjeR?= MXezNEBvVQ>? M4Pj[lQ5KGh? MlPzSG1UVw>? M4HTcGRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? M37RflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXQSG1UVw>? NX;5UG5IUUN3ME2wMlE4KM7:TR?= NHj4cpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 M3XpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO2boJRTE2VTx?= MX7JR|UxRTBwMkig{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NF\HZ4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zKbmROW09? NF3jU2pKSzVyPUCuNlIh|ryP M3TaUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549 NIHUfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH2PYhFVVOR NHfFS3lKSzVyPUCuNFQh|ryP M2q2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H358 NVLEVFlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDFUYdFVVOR MXTJR|UxRTBwMTFOwG0> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H460 NGjIPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnEUXNQ MnrzTWM2OD1yLkGzJO69VQ>? M2jWdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
CMK MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\WUmlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCZVDDKRWsh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlA4PSEQvF2= MnKwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK NIDZU4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDiTWpKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E3O0RibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjF4MzFOwG0> MlzTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK NGm5[pJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G1O|JXKG23dHH0bY9vKGOnbHygdJJwdGmoZYLheIlwdg>? M3m0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
HT93A MkXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3QUm9jOzJyIH7N MWC1JIQ> MnTTSG1UVw>? M4rBNWlvcGmkaYTpc44hd2ZiR1PTMWYhcW6mdXPl[EBoemGwdXzvZ5l1cWNiZHnm[oVz\W62aXH0bY9v MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThyNUm2Nkc,OjV6MEW5OlI9N2F-
SET-2 M1PZ[mN6fG:2b4jpZ{BCe3OjeR?= M2Loe|Uh|ryP NWe2TYp1PDhiaB?= Mkf1R5l1d3SxeHnjJIlv\GW6PUG4Mlcm M3vjbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
HEL MmS4R5l1d3SxeHnjJGF{e2G7 Mmr4OUDPxE1? MVK0PEBp M{\UTGN6fG:2b4jpZ{BqdmSneE2xNk4zLQ>? NIPhdIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmzNVM1QSd-MkW5N|E{PDl:L3G+
Human monocyte M2SyXWtqdmG|ZTDBd5NigQ>? NEj5d3hKdmirYnn0bY9vKG:oIFrBT|IwOSCrbjDoeY1idiCvb37vZ5l1\XNiZYjwdoV{e2mwZzDDSFE1KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUU[QZ3HtcYEue3SrbYXsZZRm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEOx{txO M2jnU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
Human monocyte NYDiUmE6U2mwYYPlJGF{e2G7 NEnxSFJKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGdONUOVRj3zeIlufWyjdHXkJHNVSVR3YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODJ4zszN MonJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human T cell NXjXW29LU2mwYYPlJGF{e2G7 NF20W2FKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? Mli1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
TF1 NFfu[2dMcW6jc3WgRZN{[Xl? NHXhUY0zOCCvaX6= NWDtNIJlTE2VTx?= NFWxUohKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? NHzrUm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR: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.
Animal Research:[1]
  • Animal Models: JAK2V617F-driven mouse model
  • Dosages: 180 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

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

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)

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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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