Ruxolitinib (INCB018424)

For research use only. Not for use in humans.

目录号:S1378 中文名称:鲁索替尼

Ruxolitinib (INCB018424) Chemical Structure

CAS No. 941678-49-5

Ruxolitinib (INCB018424)是第一个应用于临床的,有效的,选择性JAK1/2抑制剂,在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与作用于JAK3相比,选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1703.45 现货
RMB 1317.79 现货
RMB 2633.61 现货
RMB 6542.21 现货
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客户使用Selleck生产的Ruxolitinib (INCB018424)发表文献390篇:

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Ruxolitinib (INCB018424)是第一个应用于临床的,有效的,选择性JAK1/2抑制剂,在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与作用于JAK3相比,选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。
靶点
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
2.8 nM 3.3 nM
体外研究

在Ba/F3细胞和HEL细胞中,INCB018424有效地和有选择性地抑制JAK2V617F介导的信号传导和细胞增殖。INCB018424以剂量依赖性的方式显着地增加Ba/F3细胞的细胞凋亡。在Ba/F3细胞中,INCB018424(64 nM)致使线粒体去极化细胞增加一倍。INCB018424抑制来自正常捐助者和真性红细胞增多症患者的红细胞前体细胞的增殖,IC50分别是407 nM 和223 nM。 INCB018424有效抑制红细胞集落形成,IC50是67 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SNU423 M1vyeGZ2dmO2aX;uJGF{e2G7 NHHsUHM2OCEQvF2= NYHZZVVHOjRiaB?= M2nPdWROW09? MlOxTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M2D3dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 NYTOUoNOTnWwY4Tpc44hSXO|YYm= MnXBOVAh|ryP M2HGV|I1KGh? M{joZWROW09? Mln6TY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NXfCVXBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
HuH7 NUPUNJBtTnWwY4Tpc44hSXO|YYm= NI\4[2I2OCEQvF2= MoXiNlQhcA>? MXLEUXNQ MVfJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? M1\SblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU423 NX6zbZIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDmVoI2OCEQvF2= MVO0PEBp MmTySG1UVw>? NVv6Z|ZYRjhzJTDy[YR2[3Srb36= MmexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
SNU182 NIPLRW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe0UYU2OCEQvF2= Ml7oOFghcA>? MYLEUXNQ NF;SZlg,PjRnIILl[JVkfGmxbh?= NV\Ed2VDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
HuH7 NELD[mVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\ycZhVPTBizszN NFzGVpU1QCCq NYnEOGNJTE2VTx?= M1H0N|45OiVicnXkeYN1cW:w M2nmOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
RKO NVrpSlZpSXCxcITvd4l{KEG|c3H5 MVSyOUDPxE1? Ml;4OFghcA>? NXfZW5RzTE2VTx?= NYLmdJVtUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= NUDtU|N2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
DLD-1 MlOyRZBweHSxc3nzJGF{e2G7 M1[1RVI2KM7:TR?= M1\hZ|Q5KGh? NX[4WnN6TE2VTx?= NHPPdGxKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= Ml\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 NFTvSnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWW1NEDPxE1? M4LobVQ5KGh? NU[5cHJETE2VTx?= MWPJR|UxRTF3LkWxJO69VQ>? M{jWO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO NEPSZ4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;n[lUxKM7:TR?= NGLVToQ1QCCq M2DoNmROW09? M3W0bGlEPTB;MUSuO|Yh|ryP NYTJWJdiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO M4C5NWtqdmG|ZTDBd5NigQ>? MoC2NlUh|ryP M3[zXlQ5KGh? NYjmeY1kTE2VTx?= MoK5[I9meyCwb4SgbY5pcWKrdDDKRWsyKHCqb4PwbI9zgWyjdHnvci=> NHnQZnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 M33McWtqdmG|ZTDBd5NigQ>? NX;F[HFSOjVizszN NIHQdVg1QCCq M1zzSmROW09? M1TCXWlvcGmkaYTpc44hd2ZiSlHLNkBxcG:|cHjvdplt[XSrb36= MmXBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
RKO MUnLbY5ie2ViQYPzZZk> M{Dyb|I2KM7:TR?= NH:0fYs1QCCq NEKzWI5FVVOR NV7WV5VYUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 MWPLbY5ie2ViQYPzZZk> MXWyOUDPxE1? M2HhdlQ5KGh? NFfSfZZFVVOR MkT6TY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
BaF3 MYXLbY5ie2ViQYPzZZk> M2HsblgxKG6P NU\vfph{PiCq MnXzSG1UVw>? NVnkRVlrWmWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:owrDTWGFVPSCrbjDKRWszXjZzN1[tcZV1[XSnZDDCRWY{NUWST2KgZ4VtdA>? NV7iUGF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|c4QTFpPkK0NlM4PzlzPD;hQi=>
Huh7 MVPGeY5kfGmxbjDBd5NigQ>? MX6xJO69VQ>? MVexOkBp NF2zfWlFVVOR M324[2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> M2DTVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
HepG2 MULGeY5kfGmxbjDBd5NigQ>? M1jmWlEh|ryP M17KV|E3KGh? Mn\vSG1UVw>? M2\l[2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> MmnPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEG2PFkoRjJ2NUCxOlg6RC:jPh?=
Hep3B NVXTcZIzTnWwY4Tpc44hSXO|YYm= Ml[3NUDPxE1? NULobWdHOTZiaB?= NGLkO4RFVVOR NXv5UYl3UW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIHHjeIl3\SCVVFHUN{B4cXSqIFnDOVAhd2ZifkWwJO69VQ>? M4r4WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
NCI-H2347 Ml30RZBweHSxc3nzJGF{e2G7 M2e4TlMxKG6P M4PX[FQ5KGh? MkXOSG1UVw>? NGHYUZlKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M3jqfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 MYDBdI9xfG:|aYOgRZN{[Xl? NXe1NFhWOzBibl2= MU[0PEBp MUjEUXNQ MnTaTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NWfMfVdoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP MkHWRZBweHSxc3nzJGF{e2G7 NG\lZWs{OCCwTR?= Mne4OFghcA>? MYfEUXNQ M3X0fWlv\HWldHnvckBw\iCjcH;weI9{cXN? MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H1299 MVrGeY5kfGmxbjDBd5NigQ>? M2XEUFMxKG6P NIXzT2Y1QCCq M1rkS2ROW09? NUTCe4hrTG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= NF;FR249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H2347 NX\aZWN6TnWwY4Tpc44hSXO|YYm= MmPjN|Ahdk1? NYT4PVBSPDhiaB?= NWfGd4lxTE2VTx?= MYLE[YNz\WG|ZTDpckBD[2x{IHX4dJJme3Orb36= NH\sb2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP NGHKSpVHfW6ldHnvckBCe3OjeR?= MWOzNEBvVQ>? MlK5OFghcA>? MWLEUXNQ M{Wxc2Rwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? M4\m[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 NFzRNGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HLXGROW09? MWPJR|UxRTBwMUeg{txO MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 NVuzWJR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPsTYpFVVOR NYLrRlQ5UUN3ME2wMlI5KM7:TR?= MlyxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
A549/DDP NGjtV5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\Hb2ROW09? M4Llc2lEPTB;MD6yNkDPxE1? NH7DRXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\NSG1UVw>? MXTJR|UxRTBwMESg{txO MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H358 NXLySZhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTpSG1UVw>? NYfJbph3UUN3ME2wMlEh|ryP NXrrcFRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H460 Mn\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m3ZWROW09? Mmm5TWM2OD1yLkGzJO69VQ>? MnLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
CMK M3rEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnPTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKFeWIFrBT{Bk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFc2KM7:TR?= MnfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
CMK MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\PTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOlNFKG23dHH0bY9vKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yPjNizszN M1uxblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInIZmlKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E2PzKYIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbh?= NWOyeFd[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
HT93A NUm5T2hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPUN|IxKG6P Mn;qOUBl M{XwZmROW09? M2[0eGlvcGmkaYTpc44hd2ZiR1PTMWYhcW6mdXPl[EBoemGwdXzvZ5l1cWNiZHnm[oVz\W62aXH0bY9v NXTFXIpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NFU6PjJpPkK1PFA2QTZ{PD;hQi=>
SET-2 NYLWUmRiS3m2b4TvfIlkKEG|c3H5 M1vXc|Uh|ryP M3PEOlQ5KGh? M1n6WWN6fG:2b4jpZ{BqdmSneE2xPE44LQ>? M2TnOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
HEL M4PPfmN6fG:2b4jpZ{BCe3OjeR?= MmG2OUDPxE1? M1PQW|Q5KGh? NHvwcoVEgXSxdH;4bYMhcW6mZYi9NVIvOiV? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl|MUO0PUc,OjV7M{GzOFk9N2F-
Human monocyte MWTLbY5ie2ViQYPzZZk> M3L6N2lvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> MkPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human monocyte NYfOUo1RU2mwYYPlJGF{e2G7 NVzqRnNWUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBIVS2FU1[td5RqdXWuYYTl[EBUXEGWNXGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{Nt88US=> NV;WS5Z5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
Human T cell M3nUfGtqdmG|ZTDBd5NigQ>? NXG0fHNuUW6qaXLpeIlwdiCxZjDKRWs{NzFiaX6gbJVu[W5iVDDj[YxteyCneIDy[ZN{cW6pIFPEN{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNOi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI{|ryP M1Twe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
TF1 NVzs[np2U2mwYYPlJGF{e2G7 MmTENlAhdWmw NVf6VW97TE2VTx?= M3TISmlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEK0{txO M1TOPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nkm4NFg1Lz5{Mk[5PFA5PDxxYU6=
TF1 NHjCT|hMcW6jc3WgRZN{[Xl? M1;QXlIxKG2rbh?= MVnEUXNQ NEjuPWVKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVCRLXnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxNu69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
Sf9 cells MV7KRWshcW6qaXLpeIlwdiCjc4PhfS=> NUTGfnZnOSCq Mm\VT4khRSByLkCwNFEh|ryP NUnVblRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf9 cells MnfUTmFMKGmwaHnibZRqd25iYYPzZZk> MojRNUBp MYfLbUA:KDBwMECwNkDPxE1? NXHNdm1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf9 cells M1zEdWpCUyCrbnjpZol1cW:wIHHzd4F6 MYixJIg> NXfqUVhnU2liPTCwMlAxODVizszN Mnj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4Nki0PFQoRjJ|Nk[4OFg1RC:jPh?=
SET2 cells M1j1Z2pCUyCrbnjpZol1cW:wIHHzd4F6 NYn4b2J{UUN3MDC9JFAvODBzOESg{txO MkjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkG2OlAoRjJ|ME[xOlYxRC:jPh?=
Sf21 cells MlHkTmFMKGmwaHnibZRqd25iYYPzZZk> M3fwdFEhcA>? MnLMTWM2OCB;IECuNFAzQCEQvF2= NU[xd2VLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVE1ODJpPkKyOVkyPDB{PD;hQi=>
Sf21 cells MWXKRWshcW6qaXLpeIlwdiCjc4PhfS=> Ml3jOlAhdWmw MkPHTWM2OCB;IECuNFA{KM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|N{O1PUc,OjdzM{ezOVk9N2F-
Sf9 cells NX;vXXZoUkGNIHnubIljcXSrb36gZZN{[Xl? M3TvS|EhcA>? MXrLbUA:KDBwMECzNkDPxE1? M13NRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf21 cells MoTJTmFMKGmwaHnibZRqd25iYYPzZZk> Ml3INUBp NYPFeYI4UUN3MDC9JFAvODB|MzFOwG0> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
TF1 cells Ml[zTmFMKGmwaHnibZRqd25iYYPzZZk> NY\3NVJXOzBibXnu MnL6TWM2OCB;IECuNFA3QDVizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB4MU[2NEc,OjNyNkG2OlA9N2F-
CD34+ cells NHqy[2xLSUtiaX7obYJqfGmxbjDhd5NigQ>? NXfEWHo5UUN3MDC9JFAvODB6IN88US=> MkDZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
TF1 cells MmLhTmFMKGmwaHnibZRqd25iYYPzZZk> MY[yNEBucW5? NY\1fW9sTUN3MDC9JFAvODF{IN88US=> M3zTRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nkm4NFg1Lz5{Mk[5PFA5PDxxYU6=
Sf21 cells MWrUXWszKGmwaHnibZRqd25iYYPzZZk> M4PmTFEhcA>? NWCyXmFCUUN3MDC9JFAvODF7IN88US=> NHnMdZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
T cells M2fYN2pCUyCrbnjpZol1cW:wIHHzd4F6 MWHJR|UxKD1iMD6wNlMh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
T cells MVzKRWshcW6qaXLpeIlwdiCjc4PhfS=> M3y5VWlEPTBiPTCwMlAzOyEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 cells MoHOTmFMKGmwaHnibZRqd25iYYPzZZk> MYCyNEBucW5? MlPVSWM2OCB;IECuNFI1KM7:TR?= NGq1PI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
T cells NUD4UGQzUkGNIHnubIljcXSrb36gZZN{[Xl? NUfMU3NNUUN3MDC9JFAvODNzIN88US=> M3KzUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells MnfsTmFMKGmwaHnibZRqd25iYYPzZZk> NHWzSYZKSzVyIE2gNE4xOzFizszN MmnFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
PBMC cells M1HUeWpCUyCrbnjpZol1cW:wIHHzd4F6 NYTJZoVZUUN3MDC9JFAvODRizszN M132T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
Sf21 cells NYS4bYw3UkGNIHnubIljcXSrb36gZZN{[Xl? NHrUcW8yKGh? Ml3TTWM2OCB;IECuOFI5KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
PBMC cells NX\MT5FSW1SDVEWgbY5pcWKrdHnvckBie3OjeR?= NXLZfIEzUUN3MDC9JFAvPDR6IN88US=> M1PsS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
CD34+ cells MVzKRWshcW6qaXLpeIlwdiCjc4PhfS=> MoDHOFUhdWmw NEG1U2NKSzVyIE2gNE43PzdizszN M3PWflxiKHSjcnfleF0oZ2KuYX7rK{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
体内研究 INCB018424(180 mg/kg,口服,每日两次)导致JAK2V617F驱动的小鼠模型的生存率在处理22天后大于90%。在JAK2V617F驱动的小鼠模型中,INCB018424(180 mg/kg,口服,每日两次)显着降低脾脏肿大和炎症因子的循环水平,并优先消灭肿瘤细胞,造成显著延长的生存期,无骨髓抑制或免疫抑制作用。[1] 在骨髓纤维化的双盲试验中,Ruxolitinib组的主要终点达到41.9%,安慰剂组则为0.7%。 Ruxolitinib导致脾体积持续减少和总症状得分提高50%或更多。[2] 在Ruxolitinib(15 mg,每天两次)组内,共28%骨髓纤维化患者至48周时脾脏体积减少至少35%,而接受最好的治疗组的比例为0%。Ruxolitinib致使脾脏长度减少了56%,而接受最好的治疗组却增加了4%。Ruxolitinib组患者的生活质量得到提高和骨髓纤维化相关症状减少。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

结合试验:

重组蛋白是使用Sf21细胞和杆状病毒载体表达的,并通过亲和层析纯化。JAK激酶测定使用肽底物(-EQEDEPEGDYFEWLE)的均相时间分辨荧光测定法。酶反应是用Ruxolitinib或对照,JAK酶,500 nM肽,三磷酸腺苷(ATP; 1mM),和2%的二甲基亚砜(DMSO)反应1小时。 50%抑制浓度(IC50)时需要抑制50%荧光信号的INCB018424浓度。
细胞实验:[1]
- 合并
  • Cell lines: Ba/F3和HEL细胞
  • Concentrations: 3 μM
  • Incubation Time: 48小时
  • Method: 2×103细胞接种于的96孔板的一个孔中,用溶于DMSO的INCB018424(0.2%DMSO终浓度)在37℃和5% CO2条件下温育48小时。存活率是通过使用细胞滴度格洛荧光素酶试剂或活细胞计数器测定ATP水平。数值转换为相比对照的抑制百分率, IC50曲线使用Prism的GraphPad数据的非线性回归分析拟合。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: JAK2V617F驱动的小鼠模型
  • Dosages: 180 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 61 mg/mL (199.1 mM)
Ethanol 61 mg/mL (199.1 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 306.37
化学式

C17H18N6

CAS号 941678-49-5
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What is the difference between S2902 and S1378 which seem to have same structure formula according to the product information?

  • 回答:

    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.

  • 问题 2:

    How about the half-life of the compound (Ruxolitinib)? How long is the duration of the inhibitory effect on JAK-STAT signaling?

  • 回答:

    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.

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

相关JAK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID