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 1896.85 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361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 NHrJS4FHfW6ldHnvckBCe3OjeR?= M2HmTlUxKM7:TR?= MnfENlQhcA>? Mn\QSG1UVw>? NVT4cJBRUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NFrYNYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 NWDxTGx{TnWwY4Tpc44hSXO|YYm= M2XzZVUxKM7:TR?= M3Lmc|I1KGh? MYLEUXNQ NF3oWHVKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NVrGN5A1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
HuH7 NGfLfpJHfW6ldHnvckBCe3OjeR?= NViwOIRpPTBizszN NU\mZnV4OjRiaB?= NGXsNnlFVVOR NGnh[3NKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= NV7OOpV{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
SNU423 M1H6V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Dhc|UxKM7:TR?= MmK4OFghcA>? NX;nWoxXTE2VTx?= NV7IcYk1RjhzJTDy[YR2[3Srb36= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
SNU182 M1fReWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\3dVUxKM7:TR?= NX;idHpEPDhiaB?= NWC1NotLTE2VTx?= Mm\3QlY1LSC{ZXT1Z5Rqd25? NGHHNHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
HuH7 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHYUZM2OCEQvF2= MnnoOFghcA>? NH\BOWtFVVOR NEjWWoc,QDJnIILl[JVkfGmxbh?= NFGzV5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
RKO M4XKe2Fxd3C2b4Ppd{BCe3OjeR?= MUGyOUDPxE1? MWq0PEBp M1TjPGROW09? NIjLTWRKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCjY4TpeoF1cW6pIHPhd5Bie2ViMx?= NGW1SoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 Ml34RZBweHSxc3nzJGF{e2G7 M1n3cFI2KM7:TR?= MXq0PEBp M1e1VGROW09? M2PVVWlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NX7nSndiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LoVFUxKM7:TR?= MYC0PEBp NIfmToVFVVOR Ml\aTWM2OD1zNT61NUDPxE1? NYO3SZg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO MnXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPHOVAh|ryP MoLoOFghcA>? M1;GSmROW09? M2jUcWlEPTB;MUSuO|Yh|ryP MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
RKO NFXqU2lMcW6jc3WgRZN{[Xl? MYeyOUDPxE1? NGfiWII1QCCq NH3VTWVFVVOR MmTR[I9meyCwb4SgbY5pcWKrdDDKRWsyKHCqb4PwbI9zgWyjdHnvci=> NHfsRZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 NYTzZXIzU2mwYYPlJGF{e2G7 NFuzbpczPSEQvF2= MYq0PEBp NWGybpY1TE2VTx?= NEPDNXpKdmirYnn0bY9vKG:oIFrBT|IheGixc4Doc5J6dGG2aX;u M4THOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MWTLbY5ie2ViQYPzZZk> M1\wVFI2KM7:TR?= M2SxUFQ5KGh? MWDEUXNQ NVnxfmRrUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> NVSydWk1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
DLD-1 M1XnW2tqdmG|ZTDBd5NigQ>? MlzONlUh|ryP M17WRVQ5KGh? NXHRO2pSTE2VTx?= NVjnOm1XUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
BaF3 NUnhXlZ7U2mwYYPlJGF{e2G7 NVzCNIFsQDBibl2= MVK2JIg> MoDPSG1UVw>? NXzXNGhsWmWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:owrDTWGFVPSCrbjDKRWszXjZzN1[tcZV1[XSnZDDCRWY{NUWST2KgZ4VtdA>? NWrxfmR4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|c4QTFpPkK0NlM4PzlzPD;hQi=>
Huh7 M1\mSGZ2dmO2aX;uJGF{e2G7 MVSxJO69VQ>? Ml\ONVYhcA>? MnXwSG1UVw>? NELHVHpKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9ic3nncoFtKHSxIGPURXQ{ MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
HepG2 MkHCSpVv[3Srb36gRZN{[Xl? MUGxJO69VQ>? NVLTNJIyOTZiaB?= NVvJXmsyTE2VTx?= NWPkVXlPUW2yYXny[ZMhfGinIHPhdIFkcXS7IH;mJGlJS0FvYYPzc4Nq[XSnZDDndFE{OCCvdYThcpR{KHSxIIPp[45idCC2bzDTWGFVOw>? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
Hep3B MorwSpVv[3Srb36gRZN{[Xl? MkHVNUDPxE1? NYDmO4VpOTZiaB?= M4[wRWROW09? NEH0VIRKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9iYXP0bZZmKFOWQWSzJJdqfGhiSVO1NEBw\iC-NUCg{txO NGq0U3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
NCI-H2347 MWXBdI9xfG:|aYOgRZN{[Xl? MnK5N|Ahdk1? MXK0PEBp M1rp[WROW09? M4fjemlv\HWldHnvckBw\iCjcH;weI9{cXN? NV3EVIZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H1299 MnTxRZBweHSxc3nzJGF{e2G7 MlfhN|Ahdk1? NVXTV2t2PDhiaB?= NVnhV3ZTTE2VTx?= MXPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NIfmSJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549/DDP NH3DTXBCeG:ydH;zbZMhSXO|YYm= MYSzNEBvVQ>? MmDHOFghcA>? NFXKZnBFVVOR NYfJfWlnUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NYHIcIM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H1299 MUfGeY5kfGmxbjDBd5NigQ>? M4i4RlMxKG6P M3fiUVQ5KGh? NVGxbYM{TE2VTx?= MWDEc5dvNXKnZ4XsZZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9v MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H2347 MV7GeY5kfGmxbjDBd5NigQ>? NF\hSHg{OCCwTR?= NX;VW4xnPDhiaB?= MluwSG1UVw>? M2DSbGRm[3KnYYPlJIlvKEKlbEKg[ZhxemW|c3nvci=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP NUnoO|lZTnWwY4Tpc44hSXO|YYm= NEfMPJk{OCCwTR?= M2CzPVQ5KGh? NWSyfGJOTE2VTx?= M3fYU2Rwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? Mmq1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H2347 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf3[VdZTE2VTx?= NWHXPY1tUUN3ME2wMlE4KM7:TR?= M4r0OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 NEG2e5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr1N4FFVVOR NV\MOYR{UUN3ME2wMlI5KM7:TR?= M4Sz[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fhbmROW09? MmK3TWM2OD1yLkKyJO69VQ>? NWG4boM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549 NIXPSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjjSG1UVw>? MmXYTWM2OD1yLkC0JO69VQ>? NUXOVZdtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H358 NH\HTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{na[mROW09? NIqxTFZKSzVyPUCuNUDPxE1? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H460 NXH6b2Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLEUXNQ M{KzNmlEPTB;MD6xN{DPxE1? M1q0Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
CMK M{\1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjSSoxUUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=> NY\rWm5JRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOVIyOjRpPkK1N|UzOTJ2PD;hQi=>
CMK MlnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\Jcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G2N2QhdXW2YYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlE3OyEQvF2= M2SyclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK NXTD[YU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfJdXZKdmirYnn0bY9vKG:oIFPNT{Bk[XK{eXnu[{B1cGViSlHLN2E2PzKYIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbh?= MlnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
HT93A MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLpN|IxKG6P M3TGOFUh\A>? MWXEUXNQ NHG3NGNKdmirYnn0bY9vKG:oIFfDV{1HKGmwZIXj[YQh\3KjboXsc4N6fGmlIHTp[oZmemWwdHnheIlwdg>? M{\4b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEC1PVYzLz5{NUiwOVk3OjxxYU6=
SET-2 M1zQbmN6fG:2b4jpZ{BCe3OjeR?= M3y0XVUh|ryP Mli5OFghcA>? NH[xR5BEgXSxdH;4bYMhcW6mZYi9NVgvPyV? NUHEVIFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|E{PDlpPkK1PVMyOzR7PD;hQi=>
HEL M3vtOGN6fG:2b4jpZ{BCe3OjeR?= MmPmOUDPxE1? MnHROFghcA>? M3TUUGN6fG:2b4jpZ{BqdmSneE2xNk4zLQ>? M{ny[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
Human monocyte M4XmRmtqdmG|ZTDBd5NigQ>? MWLJcohq[mm2aX;uJI9nKEqDS{KvNUBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWZP\2GvbXGtd5RqdXWuYYTl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODNzzszN MnPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human monocyte NVnoU|NvU2mwYYPlJGF{e2G7 NEHMNG1KdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hdW:wb3P5eIV{KGW6cILld5NqdmdiQ1SxOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGdONUOVRj3zeIlufWyjdHXkJHNVSVR3YTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODJ4zszN NXLuOZRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
Human T cell M2j1dmtqdmG|ZTDBd5NigQ>? MWjJcohq[mm2aX;uJI9nKEqDS{OvNUBqdiCqdX3hckBVKGOnbHzzJIV5eHKnc4PpcochS0R|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVyyMZN1cW23bHH0[YQhW1SDVEXhJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkROwG0> MkXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
TF1 M{LjfWtqdmG|ZTDBd5NigQ>? M1XGflIxKG2rbh?= MXLEUXNQ MmjETY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkVOwG0> NGP5N489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
TF1 NGmwcppMcW6jc3WgRZN{[Xl? NIjhbogzOCCvaX6= MlPZSG1UVw>? Ml3kTY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWS1JJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMUNOwG0> M{\zeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nkm4NFg1Lz5{Mk[5PFA5PDxxYU6=
Sf9 cells Ml\YTmFMKGmwaHnibZRqd25iYYPzZZk> MW[xJIg> M4iycmtqKD1iMD6wNFAyKM7:TR?= M4rUR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf9 cells MVjKRWshcW6qaXLpeIlwdiCjc4PhfS=> NUTNeo5EOSCq MYXLbUA:KDBwMECwNkDPxE1? NWKxb29kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2Olg1QDRpPkKzOlY5PDh2PD;hQi=>
Sf9 cells MU\KRWshcW6qaXLpeIlwdiCjc4PhfS=> NYrRdXJjOSCq M1ryUWtqKD1iMD6wNFA2KM7:TR?= NGTjRWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2PFQ5PCd-MkO2Olg1QDR:L3G+
SET2 cells M3[yVmpCUyCrbnjpZol1cW:wIHHzd4F6 NWLWbpk{UUN3MDC9JFAvODBzOESg{txO NFGzbFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C2NVY3OCd-MkOwOlE3PjB:L3G+
Sf21 cells NEfkSFBLSUtiaX7obYJqfGmxbjDhd5NigQ>? MmjiNUBp M{PZ[WlEPTBiPTCwMlAxOjhizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
Sf21 cells M1:3eGpCUyCrbnjpZol1cW:wIHHzd4F6 MWS2NEBucW5? NHTvdm1KSzVyIE2gNE4xODNizszN MnPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{ezOVkoRjJ5MUO3N|U6RC:jPh?=
Sf9 cells NXPqZ5R2UkGNIHnubIljcXSrb36gZZN{[Xl? MXGxJIg> Ml\FT4khRSByLkCwN|Ih|ryP MoThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4Nki0PFQoRjJ|Nk[4OFg1RC:jPh?=
Sf21 cells M2PNdmpCUyCrbnjpZol1cW:wIHHzd4F6 NFHudncyKGh? M2LBWGlEPTBiPTCwMlAxOzNizszN M3;GZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUmxOFAzLz5{MkW5NVQxOjxxYU6=
TF1 cells MUnKRWshcW6qaXLpeIlwdiCjc4PhfS=> MY[zNEBucW5? NWjyVHViUUN3MDC9JFAvODB4OEWg{txO MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB4MU[2NEc,OjNyNkG2OlA9N2F-
CD34+ cells M{H5NmpCUyCrbnjpZol1cW:wIHHzd4F6 NXPnUmVxUUN3MDC9JFAvODB6IN88US=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{N{SyN{c,OjZ7Mke0NlM9N2F-
TF1 cells MUPKRWshcW6qaXLpeIlwdiCjc4PhfS=> NILh[IQzOCCvaX6= MkPOSWM2OCB;IECuNFEzKM7:TR?= MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
Sf21 cells NXTWbWl[XFmNMjDpcohq[mm2aX;uJIF{e2G7 MlmyNUBp MYLJR|UxKD1iMD6wNVkh|ryP Ml3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3OUG0NFIoRjJ{NUmxOFAzRC:jPh?=
T cells NULGOYIzUkGNIHnubIljcXSrb36gZZN{[Xl? NUfPU2VTUUN3MDC9JFAvODJ|IN88US=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
T cells NUfqO5FVUkGNIHnubIljcXSrb36gZZN{[Xl? Mli0TWM2OCB;IECuNFI{KM7:TR?= NHjje3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
TF1 cells NYniWopbUkGNIHnubIljcXSrb36gZZN{[Xl? NGLTTZEzOCCvaX6= NUKwVIlLTUN3MDC9JFAvODJ2IN88US=> NH[xN4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
T cells M3\xUGpCUyCrbnjpZol1cW:wIHHzd4F6 NXXXfJVOUUN3MDC9JFAvODNzIN88US=> NGq2UGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
T cells MXrKRWshcW6qaXLpeIlwdiCjc4PhfS=> NWf6[mtmUUN3MDC9JFAvODNzIN88US=> M3HVZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
PBMC cells M1LHR2pCUyCrbnjpZol1cW:wIHHzd4F6 M2DKWmlEPTBiPTCwMlA1KM7:TR?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{N{SyN{c,OjZ7Mke0NlM9N2F-
Sf21 cells M1naVGpCUyCrbnjpZol1cW:wIHHzd4F6 NUTSXI57OSCq MXvJR|UxKD1iMD60Nlgh|ryP NYHNbmpZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVE1ODJpPkKyOVkyPDB{PD;hQi=>
PBMC cells MVzTWGFVPSCrbnjpZol1cW:wIHHzd4F6 MWnJR|UxKD1iMD60OFgh|ryP MmnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
CD34+ cells MUfKRWshcW6qaXLpeIlwdiCjc4PhfS=> NFrFZWQ1PSCvaX6= MV;JR|UxKD1iMD62O|ch|ryP M4\Vb|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、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 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

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