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409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 NXz2W|I2TnWwY4Tpc44hSXO|YYm= MmLLOVAh|ryP MUmyOEBp NXTMeHlXTE2VTx?= Mm\jTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? M2L2NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUSxPFMzLz5{M{m0NVg{OjxxYU6=
SNU182 MmDJSpVv[3Srb36gRZN{[Xl? M{HqTlUxKM7:TR?= NInZfo0zPCCq NU\kVFhKTE2VTx?= MoPOTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MmC1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
HuH7 NFrNWmxHfW6ldHnvckBCe3OjeR?= NFv1TWc2OCEQvF2= M{XIVVI1KGh? MYfEUXNQ MmHvTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? NVqyUmRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU423 NV7iWXh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfnUWY2OCEQvF2= MX:0PEBp NG\4cZFFVVOR NUHtZYVtRjhzJTDy[YR2[3Srb36= NH\afo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 NHmybXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjkUoI5PTBizszN NVHwb2o5PDhiaB?= MXPEUXNQ NVT0[FFVRjZ2JTDy[YR2[3Srb36= NF3mRYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 NVL6TIFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfwOVAh|ryP MYG0PEBp NEf1NHhFVVOR NXLjUYF5Rjh{JTDy[YR2[3Srb36= Mke5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
RKO MXnBdI9xfG:|aYOgRZN{[Xl? NYfFbFhKOjVizszN NY\jbG1qPDhiaB?= NYS2VmhuTE2VTx?= NYK4cWQ4UW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= MnHjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 MVHBdI9xfG:|aYOgRZN{[Xl? NEHKNoIzPSEQvF2= MnTjOFghcA>? NWfUSWdSTE2VTx?= NXrLV3BXUW6mdXPld{BieG:ydH;zbZMh[nliYXP0bZZifGmwZzDjZZNx[XOnIEO= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NGHYWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3GbFY{PTBizszN NYrRO21XPDhiaB?= NInTW5ZFVVOR MXTJR|UxRTF3LkWxJO69VQ>? M2WxV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO NGrVPIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[1NEDPxE1? NEGzdJo1QCCq Mm[3SG1UVw>? NHT6fFhKSzVyPUG0Mlc3KM7:TR?= NX\2cpp7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO M2\hS2tqdmG|ZTDBd5NigQ>? M160V|I2KM7:TR?= M3PsTlQ5KGh? MYrEUXNQ M4DQ[4Rw\XNibn;0JIlvcGmkaYSgTmFMOSCyaH;zdIhwenmuYYTpc44> M2e3clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 NXPFd3JRU2mwYYPlJGF{e2G7 NE[yNZMzPSEQvF2= M4LqN|Q5KGh? Ml32SG1UVw>? M{HreGlvcGmkaYTpc44hd2ZiSlHLNkBxcG:|cHjvdplt[XSrb36= MmjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
RKO MXTLbY5ie2ViQYPzZZk> NHPYWIUzPSEQvF2= MWS0PEBp MUDEUXNQ MXXJcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w M12weVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 MmLvT4lv[XOnIFHzd4F6 MlnUNlUh|ryP MWK0PEBp MkLISG1UVw>? NHjGOoZKdmirYnn0bY9vKG:oIFrBT|EheGixc4Doc5J6dGG2aX;u MnHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
BaF3 NULiNnFMU2mwYYPlJGF{e2G7 MoG4PFAhdk1? MlHlOkBp MWfEUXNQ NU\zNVZIWmWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:owrDTWGFVPSCrbjDKRWszXjZzN1[tcZV1[XSnZDDCRWY{NUWST2KgZ4VtdA>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ|N{e5NUc,OjR{M{e3PVE9N2F-
Huh7 NELFWINHfW6ldHnvckBCe3OjeR?= NITxUJcyKM7:TR?= MXexOkBp MWHEUXNQ M3nQV2lueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> NFznN|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
HepG2 M{DufWZ2dmO2aX;uJGF{e2G7 NXftTpMxOSEQvF2= M4TNT|E3KGh? M3m2cGROW09? M1\iWWlueGGrcnXzJJRp\SClYYDhZ4l1gSCxZjDJTGNCNWG|c3;jbYF1\WRiZ4CxN|AhdXW2YX70d{B1dyC|aXfuZYwhfG9iU2TBWFM> M2TTT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
Hep3B NVryWJl{TnWwY4Tpc44hSXO|YYm= MVuxJO69VQ>? M{jsXFE3KGh? MnLCSG1UVw>? NXXzSFdwUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIHHjeIl3\SCVVFHUN{B4cXSqIFnDOVAhd2ZifkWwJO69VQ>? Mo\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEG2PFkoRjJ2NUCxOlg6RC:jPh?=
NCI-H2347 MU\BdI9xfG:|aYOgRZN{[Xl? M3eyVVMxKG6P Mn;3OFghcA>? Mn7NSG1UVw>? M{\1[Wlv\HWldHnvckBw\iCjcH;weI9{cXN? NHfNTnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 NF\WOY1CeG:ydH;zbZMhSXO|YYm= MXKzNEBvVQ>? M1\yNFQ5KGh? M1HrXGROW09? NYjxeHg3UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= Ml3DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
A549/DDP NGTRWHNCeG:ydH;zbZMhSXO|YYm= MVizNEBvVQ>? MYO0PEBp NYfQcmF6TE2VTx?= MUPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 MUnGeY5kfGmxbjDBd5NigQ>? M1fjNVMxKG6P MYC0PEBp M2HHV2ROW09? NHi4XVFFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H2347 MYTGeY5kfGmxbjDBd5NigQ>? MUizNEBvVQ>? MoOwOFghcA>? MlXaSG1UVw>? Mn;aSIVkemWjc3WgbY4hSmOuMjDlfJBz\XO|aX;u MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NILVOVZHfW6ldHnvckBCe3OjeR?= NXH3VFNsOzBibl2= M1PpelQ5KGh? MnfQSG1UVw>? MUTEc5dvNXKnZ4XsZZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9v M4LneFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 MnfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\DSG1UVw>? NFPoTmhKSzVyPUCuNVch|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\McGROW09? NYPMOYhrUUN3ME2wMlI5KM7:TR?= M3nNclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP M3\IfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHq0NGxFVVOR NHLPUGFKSzVyPUCuNlIh|ryP M2rYOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549 NFWxWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULEUXNQ MoHVTWM2OD1yLkC0JO69VQ>? NWTRdXNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H358 M4nRcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjCSG1UVw>? NFv1UXJKSzVyPUCuNUDPxE1? M{fTflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H460 NHzSOG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGOyN5VFVVOR MUnJR|UxRTBwMUOg{txO NFK0doc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
CMK M3q2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\Jcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhX1RiSlHLJINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiMD6wO|Uh|ryP M1nKeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK NXj0U2V6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr6dYFKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E3O0RibYX0ZZRqd25iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjF4MzFOwG0> NYLIdIxGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
CMK MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInKZ3lKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E2PzKYIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MkGyOEc,OjV|NUKxNlQ9N2F-
HT93A MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j1W|MzOCCwTR?= NWL2WHRZPSCm NV\FSYFYTE2VTx?= MVnJcohq[mm2aX;uJI9nKEeFUz3GJIlv\HWlZXSg[5JidnWub3P5eIlkKGSrZn\ldoVvfGmjdHnvci=> Ml\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW5OlIoRjJ3OEC1PVYzRC:jPh?=
SET-2 M2fuVGN6fG:2b4jpZ{BCe3OjeR?= Mkf6OUDPxE1? MnPjOFghcA>? NVzrcW9ES3m2b4TvfIlkKGmwZHX4QVE5Njdn NWfBZ5h2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|E{PDlpPkK1PVMyOzR7PD;hQi=>
HEL MVvDfZRwfG:6aXOgRZN{[Xl? MlXsOUDPxE1? NYPtW2JCPDhiaB?= M2nHRmN6fG:2b4jpZ{BqdmSneE2xNk4zLQ>? NEHOV5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmzNVM1QSd-MkW5N|E{PDl:L3G+
Human monocyte NVPmSZFNU2mwYYPlJGF{e2G7 NYX3dlVlUW6qaXLpeIlwdiCxZjDKRWszNzFiaX6gbJVu[W5ibX;uc4N6fGW|IHX4dJJme3OrbnegR2QyPCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEmITnfhcY1iNXO2aX31cIF1\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCzNe69VQ>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
Human monocyte Mlq5T4lv[XOnIFHzd4F6 MorOTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJI1wdm:leYTld{BmgHC{ZYPzbY5oKEOGMUSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0Zvc4TpcZVt[XSnZDDTWGFVPWFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAzPs7:TR?= M4m3NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
Human T cell NGPwV2RMcW6jc3WgRZN{[Xl? MWPJcohq[mm2aX;uJI9nKEqDS{OvNUBqdiCqdX3hckBVKGOnbHzzJIV5eHKnc4PpcochS0R|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVyyMZN1cW23bHH0[YQhW1SDVEXhJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkROwG0> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 M3PLcmtqdmG|ZTDBd5NigQ>? NET6fXgzOCCvaX6= NF\kdoVFVVOR NIHWXYNKdmirYnn0bY9vKG:oIFrBT|EhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUUx4LXnu[JVk\WRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyOO69VQ>? NFHGWpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
TF1 MWLLbY5ie2ViQYPzZZk> M4e0NVIxKG2rbh?= MmHBSG1UVw>? NFjSOJBKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVCRLXnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxNu69VQ>? Mn;0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
Sf9 cells NH7MOJRLSUtiaX7obYJqfGmxbjDhd5NigQ>? M{HWblEhcA>? MWjLbUA:KDBwMECwNUDPxE1? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
Sf9 cells NEfIN2RLSUtiaX7obYJqfGmxbjDhd5NigQ>? NF\sUFIyKGh? NX62e4VXU2liPTCwMlAxODJizszN MkTyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4Nki0PFQoRjJ|Nk[4OFg1RC:jPh?=
Sf9 cells M4K0UGpCUyCrbnjpZol1cW:wIHHzd4F6 M1zzVlEhcA>? NX;tWpNWU2liPTCwMlAxODVizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
SET2 cells M1\5XWpCUyCrbnjpZol1cW:wIHHzd4F6 MonMTWM2OCB;IECuNFAyQDRizszN MoHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkG2OlAoRjJ|ME[xOlYxRC:jPh?=
Sf21 cells NITvdJBLSUtiaX7obYJqfGmxbjDhd5NigQ>? MWKxJIg> MlL5TWM2OCB;IECuNFAzQCEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
Sf21 cells NX\jZ4drUkGNIHnubIljcXSrb36gZZN{[Xl? M2HKT|YxKG2rbh?= MVjJR|UxKD1iMD6wNFMh|ryP Mn\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{ezOVkoRjJ5MUO3N|U6RC:jPh?=
Sf9 cells Mn20TmFMKGmwaHnibZRqd25iYYPzZZk> MVyxJIg> NYH0[GtDU2liPTCwMlAxOzJizszN NYO3U2tXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf21 cells NIXXXVBLSUtiaX7obYJqfGmxbjDhd5NigQ>? MWixJIg> M{mw[2lEPTBiPTCwMlAxOzNizszN NH24XXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
TF1 cells NXXGN292UkGNIHnubIljcXSrb36gZZN{[Xl? NWjqdpdKOzBibXnu MnTwTWM2OCB;IECuNFA3QDVizszN M{PRUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|ME[xOlYxLz5{M{C2NVY3ODxxYU6=
CD34+ cells MUnKRWshcW6qaXLpeIlwdiCjc4PhfS=> M3zS[GlEPTBiPTCwMlAxQCEQvF2= NIq5[mw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyO|QzOyd-Mk[5Nlc1OjN:L3G+
TF1 cells MXfKRWshcW6qaXLpeIlwdiCjc4PhfS=> NVq0W4M4OjBibXnu M2nXWWVEPTBiPTCwMlAyOiEQvF2= NWnM[ZBNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PVgxQDRpPkKyOlk5ODh2PD;hQi=>
Sf21 cells NEfab2NVYUt{IHnubIljcXSrb36gZZN{[Xl? NX:wSHpkOSCq MorHTWM2OCB;IECuNFE6KM7:TR?= MmXPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3OUG0NFIoRjJ{NUmxOFAzRC:jPh?=
T cells NFTsXYhLSUtiaX7obYJqfGmxbjDhd5NigQ>? NH3hU5dKSzVyIE2gNE4xOjNizszN MlK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
T cells NXe5ZmNnUkGNIHnubIljcXSrb36gZZN{[Xl? MWXJR|UxKD1iMD6wNlMh|ryP NVvZbYNURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
TF1 cells MUPKRWshcW6qaXLpeIlwdiCjc4PhfS=> MYeyNEBucW5? NVqycHZiTUN3MDC9JFAvODJ2IN88US=> MmG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
T cells NEfuZWNLSUtiaX7obYJqfGmxbjDhd5NigQ>? NVvJdGY3UUN3MDC9JFAvODNzIN88US=> M{DMb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells NEHBV2JLSUtiaX7obYJqfGmxbjDhd5NigQ>? NU\EZo9sUUN3MDC9JFAvODNzIN88US=> NGTqOI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
PBMC cells MX3KRWshcW6qaXLpeIlwdiCjc4PhfS=> M1nseWlEPTBiPTCwMlA1KM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{N{SyN{c,OjZ7Mke0NlM9N2F-
Sf21 cells Moi5TmFMKGmwaHnibZRqd25iYYPzZZk> M1[wd|EhcA>? MkfsTWM2OCB;IECuOFI5KM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
PBMC cells NGrBS5BUXEGWNTDpcohq[mm2aX;uJIF{e2G7 MULJR|UxKD1iMD60OFgh|ryP NFvlV|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmyO|QzOyd-Mk[5Nlc1OjN:L3G+
CD34+ cells Mo\RTmFMKGmwaHnibZRqd25iYYPzZZk> NIXVSI41PSCvaX6= NF7hWnNKSzVyIE2gNE43PzdizszN M1XTV|xiKHSjcnfleF0oZ2KuYX7rK{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、SDS / 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、SDS / 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
NCT04908735 Recruiting Drug: Ruxolitinib Hematopoietic Stem Cell Transplant (HSCT)|Bronchiolitis Obliterans (BO) Children''s Hospital Medical Center Cincinnati September 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 July 13 2021 Phase 1|Phase 2
NCT04543279 Recruiting Drug: Fostamatinib|Drug: Ruxolitinib Myelofibrosis Washington University School of Medicine|Rigel Pharmaceuticals May 3 2021 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

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