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449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 MVfGeY5kfGmxbjDBd5NigQ>? MkT1OVAh|ryP M4THelI1KGh? NFfaS5JFVVOR NVTUW2VnUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NGTRVGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 Mk\xSpVv[3Srb36gRZN{[Xl? MYi1NEDPxE1? MViyOEBp MUTEUXNQ M17XcmlvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
HuH7 NX23U5NjTnWwY4Tpc44hSXO|YYm= NHfXRmw2OCEQvF2= M1O1clI1KGh? MoG1SG1UVw>? NFPaNohKdmirYnn0bY9vKG:oIGPURXQyKGGwZDDTWGFVOyCyaH;zdIhwenmuYYTpc44he2mpbnnmbYNidnSueR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
SNU423 M3rncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHWfpRDPTBizszN NF7iVWI1QCCq MmnHSG1UVw>? NXHvUYUxRjhzJTDy[YR2[3Srb36= NHPre2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 M2DT[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInYe3A2OCEQvF2= NH:ybnk1QCCq MXnEUXNQ MUe+OlQmKHKnZIXjeIlwdg>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
HuH7 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV21NEDPxE1? M1qyR|Q5KGh? NWL3U3ZWTE2VTx?= MWG+PFImKHKnZIXjeIlwdg>? NYLoXlVLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFE5OzJpPkKzPVQyQDN{PD;hQi=>
RKO NEP3[GtCeG:ydH;zbZMhSXO|YYm= MYqyOUDPxE1? M{DNdlQ5KGh? NV\I[4JDTE2VTx?= MmXJTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? NFqwV4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
DLD-1 NUHwUJBFSXCxcITvd4l{KEG|c3H5 MX:yOUDPxE1? MUm0PEBp Mk\PSG1UVw>? MXrJcoR2[2W|IHHwc5B1d3OrczDifUBi[3SrdnH0bY5oKGOjc4Dhd4UhOw>? Mk[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 M1LjNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DpZlUxKM7:TR?= MkLaOFghcA>? NFLLWmpFVVOR Mn7XTWM2OD1zNT61NUDPxE1? NFTENXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC1NFU2OCd-MkSwOVA2PTB:L3G+
RKO MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1:2dFUxKM7:TR?= MYS0PEBp MV;EUXNQ MXTJR|UxRTF2Lke2JO69VQ>? M33QVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO NGGwVnZMcW6jc3WgRZN{[Xl? MXuyOUDPxE1? NGLDW4s1QCCq NFLEbXFFVVOR NYH5dXlx\G:nczDuc5QhcW6qaXLpeEBLSUtzIIDoc5NxcG:{eXzheIlwdg>? M3XnbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 MYrLbY5ie2ViQYPzZZk> M37yOlI2KM7:TR?= NHXNTHA1QCCq M1i5WWROW09? MXPJcohq[mm2aX;uJI9nKEqDS{KgdIhwe3Cqb4L5cIF1cW:w M{\4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MXfLbY5ie2ViQYPzZZk> NH3SNJozPSEQvF2= NVrhNpY4PDhiaB?= MYrEUXNQ M3fFWmlvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36= Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 M1jlWWtqdmG|ZTDBd5NigQ>? MlfZNlUh|ryP NF7qNHo1QCCq NFL4N3NFVVOR NVz4[nB6UW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
BaF3 MVTLbY5ie2ViQYPzZZk> MYS4NEBvVQ>? NEnWR2w3KGh? Mmf2SG1UVw>? MnHnVoVlfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJI9nyqCVVFHUOUBqdiCMQVuyWlYyP0ZvbYX0ZZRm\CCEQV[zMWVRV1JiY3XscC=> NVi5c2JMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyN|c4QTFpPkK0NlM4PzlzPD;hQi=>
Huh7 NV\zdpMzTnWwY4Tpc44hSXO|YYm= M2fGPVEh|ryP MV[xOkBp M13wZ2ROW09? MX7JcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
HepG2 NU[0dXJ[TnWwY4Tpc44hSXO|YYm= NIrxTWgyKM7:TR?= NVPzNph7OTZiaB?= MmPqSG1UVw>? Mo\UTY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKHOrZ37hcEB1dyCVVFHUNy=> M1;jclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
Hep3B MkXTSpVv[3Srb36gRZN{[Xl? MW[xJO69VQ>? MYmxOkBp NH7UXGtFVVOR MnvFTY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKGGldHn2[UBUXEGWMzD3bZRpKEmFNUCgc4YhhjVyIN88US=> Mm\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR3MEG2PFkoRjJ2NUCxOlg6RC:jPh?=
NCI-H2347 MVTBdI9xfG:|aYOgRZN{[Xl? M1fhSFMxKG6P M2rUfFQ5KGh? MXrEUXNQ MUPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NHnwWI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 NVXv[nh1SXCxcITvd4l{KEG|c3H5 MYKzNEBvVQ>? NEG2VWw1QCCq NYLkWHRpTE2VTx?= Mn7wTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP M2\4RmFxd3C2b4Ppd{BCe3OjeR?= MnnEN|Ahdk1? M3v6V|Q5KGh? M2XnVWROW09? MWPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NYrwW5lSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H1299 M{fXU2Z2dmO2aX;uJGF{e2G7 MkKxN|Ahdk1? M2H2UFQ5KGh? NITVfVFFVVOR NIP2NXRFd3ewLYLl[5Vt[XSrb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H2347 NWq1SGJbTnWwY4Tpc44hSXO|YYm= MnjVN|Ahdk1? NGXD[ok1QCCq NXrzNFV2TE2VTx?= NFHmfm1F\WO{ZXHz[UBqdiCEY3yyJIV5eHKnc4Ppc44> NULtSoVYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP NWDB[o51TnWwY4Tpc44hSXO|YYm= NYTZemczOzBibl2= M{nSVlQ5KGh? M3n5OmROW09? M1XUVGRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? M4fRVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H2347 NF\abFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr6S2lCTE2VTx?= M2rNXmlEPTB;MD6xO{DPxE1? M2DGdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
NCI-H1299 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnEUXNQ NVPuboxzUUN3ME2wMlI5KM7:TR?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
A549/DDP MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUD1[2VMTE2VTx?= NF3yWIdKSzVyPUCuNlIh|ryP NWrBSJl6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549 NIe1[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\tXWROW09? NULDfmhTUUN3ME2wMlA1KM7:TR?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H358 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTreI9FVVOR MkDaTWM2OD1yLkGg{txO NYrCO|B3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H460 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2j0ZmROW09? NUHnRpVYUUN3ME2wMlE{KM7:TR?= NUjXV4VXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
CMK NInJVG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13jcGlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCZVDDKRWsh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlA4PSEQvF2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MkGyOEc,OjV|NUKxNlQ9N2F-
CMK MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJcohq[mm2aX;uJI9nKEOPSzDjZZJzgWmwZzD0bIUhUkGNM1G2N2QhdXW2YYTpc44h[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCwMlE3OyEQvF2= M37lflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK Mn7GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq0[mtEUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPTd{VjDteZRifGmxbjDj[YxtKHC{b3zp[oVz[XSrb36= Mo\TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUKxNlQoRjJ3M{WyNVI1RC:jPh?=
HT93A NVPnWHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlj5N|IxKG6P MX61JIQ> NH;CTVhFVVOR MnP6TY5pcWKrdHnvckBw\iCJQ2OtSkBqdmS3Y3XkJIdz[W63bH;jfZRq[yCmaX\m[ZJmdnSrYYTpc44> MorJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MEW5OlIoRjJ3OEC1PVYzRC:jPh?=
SET-2 NHKxfIVEgXSxdH;4bYMhSXO|YYm= MmO4OUDPxE1? NV3BPHN4PDhiaB?= NVLQXJQ2S3m2b4TvfIlkKGmwZHX4QVE5Njdn Mn22QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{GzOFkoRjJ3OUOxN|Q6RC:jPh?=
HEL NFqzVWFEgXSxdH;4bYMhSXO|YYm= NWjUfXNWPSEQvF2= M2Lne|Q5KGh? NH3HTmNEgXSxdH;4bYMhcW6mZYi9NVIvOiV? M4rIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
Human monocyte M3exeWtqdmG|ZTDBd5NigQ>? M4HWOmlvcGmkaYTpc44hd2ZiSlHLNk8yKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKTk6pYX3tZU1{fGmvdXzheIVlKFOWQWSxJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{JOwG0> M2jZNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
Human monocyte MV;LbY5ie2ViQYPzZZk> MVPJcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gcY9vd2O7dHXzJIV5eHKnc4PpcochS0RzNDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFfNMWNUTi2|dHnteYxifGWmIGPURXQ2[SCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFI3|ryP NUS4eWJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
Human T cell MWnLbY5ie2ViQYPzZZk> NFLrc|dKdmirYnn0bY9vKG:oIFrBT|MwOSCrbjDoeY1idiCWIHPlcIx{KGW6cILld5NqdmdiQ1SzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwzNXO2aX31cIF1\WRiU2TBWFViKHCqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNlPPxE1? NY\oepU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
TF1 MlTpT4lv[XOnIFHzd4F6 NWPQWW43OjBibXnu MlLWSG1UVw>? M4jaVGlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEK0{txO MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
TF1 M3PmW2tqdmG|ZTDBd5NigQ>? MmHvNlAhdWmw MomzSG1UVw>? M37uS2lvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBGWE9vaX7keYNm\CCVVFHUOUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEGy{txO MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ7OEC4OEc,OjJ4OUiwPFQ9N2F-
Sf9 cells NInIOHZLSUtiaX7obYJqfGmxbjDhd5NigQ>? NWnBXlRkOSCq MlfLT4khRSByLkCwNFEh|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
Sf9 cells NVLtbZVOUkGNIHnubIljcXSrb36gZZN{[Xl? MVKxJIg> M3LPS2tqKD1iMD6wNFAzKM7:TR?= M{jqeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf9 cells M2TIZ2pCUyCrbnjpZol1cW:wIHHzd4F6 NFnmd3AyKGh? MYXLbUA:KDBwMECwOUDPxE1? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
SET2 cells MWLKRWshcW6qaXLpeIlwdiCjc4PhfS=> NVXFdJFiUUN3MDC9JFAvODBzOESg{txO M3TqfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|ME[xOlYxLz5{M{C2NVY3ODxxYU6=
Sf21 cells NF3iOIJLSUtiaX7obYJqfGmxbjDhd5NigQ>? MVexJIg> NXvkeGRMUUN3MDC9JFAvODB{ODFOwG0> NVXvNJkyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVE1ODJpPkKyOVkyPDB{PD;hQi=>
Sf21 cells NYntOnM1UkGNIHnubIljcXSrb36gZZN{[Xl? MYK2NEBucW5? MUPJR|UxKD1iMD6wNFMh|ryP Mn\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzM{ezOVkoRjJ5MUO3N|U6RC:jPh?=
Sf9 cells NH3jbVBLSUtiaX7obYJqfGmxbjDhd5NigQ>? MYGxJIg> NH;tNHBMcSB;IECuNFA{OiEQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
Sf21 cells NETmOJJLSUtiaX7obYJqfGmxbjDhd5NigQ>? NFHzU|gyKGh? NXHNe5BUUUN3MDC9JFAvODB|MzFOwG0> M33qUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUmxOFAzLz5{MkW5NVQxOjxxYU6=
TF1 cells MkjwTmFMKGmwaHnibZRqd25iYYPzZZk> MW[zNEBucW5? NWT0W2xTUUN3MDC9JFAvODB4OEWg{txO MoX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkG2OlAoRjJ|ME[xOlYxRC:jPh?=
CD34+ cells NH:xcJZLSUtiaX7obYJqfGmxbjDhd5NigQ>? NUn2eVVjUUN3MDC9JFAvODB6IN88US=> NX[wdoRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5Nlc1OjNpPkK2PVI4PDJ|PD;hQi=>
TF1 cells NULYRnBKUkGNIHnubIljcXSrb36gZZN{[Xl? NIDNSnIzOCCvaX6= MUDFR|UxKD1iMD6wNVIh|ryP NInobpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
Sf21 cells NELWe4dVYUt{IHnubIljcXSrb36gZZN{[Xl? M{T4VVEhcA>? MmrETWM2OCB;IECuNFE6KM7:TR?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
T cells MkLNTmFMKGmwaHnibZRqd25iYYPzZZk> NHHzcmFKSzVyIE2gNE4xOjNizszN MojaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
T cells MUjKRWshcW6qaXLpeIlwdiCjc4PhfS=> MnK2TWM2OCB;IECuNFI{KM7:TR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
TF1 cells NHXaWJZLSUtiaX7obYJqfGmxbjDhd5NigQ>? NUfWUWZYOjBibXnu NFHJOlBGSzVyIE2gNE4xOjRizszN NULNWI9zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2PVgxQDRpPkKyOlk5ODh2PD;hQi=>
T cells NGXMcoZLSUtiaX7obYJqfGmxbjDhd5NigQ>? NUDzVGlDUUN3MDC9JFAvODNzIN88US=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
T cells M{jkcGpCUyCrbnjpZol1cW:wIHHzd4F6 NEPyOXJKSzVyIE2gNE4xOzFizszN MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
PBMC cells NHnN[W5LSUtiaX7obYJqfGmxbjDhd5NigQ>? M4jVTWlEPTBiPTCwMlA1KM7:TR?= M2rxcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
Sf21 cells M4XHfmpCUyCrbnjpZol1cW:wIHHzd4F6 MmLUNUBp MmfiTWM2OCB;IECuOFI5KM7:TR?= NILCOIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
PBMC cells NGXDdIhUXEGWNTDpcohq[mm2aX;uJIF{e2G7 NX7sNWY2UUN3MDC9JFAvPDR6IN88US=> M4HDclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUK3OFI{Lz5{NkmyO|QzOzxxYU6=
CD34+ cells NVzqc5h{UkGNIHnubIljcXSrb36gZZN{[Xl? NVX3VHFLPDVibXnu M37HSGlEPTBiPTCwMlY4PyEQvF2= NIfadVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U{Oyd-MkS0NVc2OzN:L3G+

... 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 只
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
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

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.

Selleck产品目录册

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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  • Tofacitinib (CP-690550) Citrate

    Tofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。

  • Tofacitinib (CP-690550)

    Tofacitinib (CP-690550,Tasocitinib)是一种新型JAK3抑制剂，在无细胞试验中IC50为1 nM，作用于JAK2和JAK1选择性低20到100倍。Tofacitinib 可在人类浆细胞样树突状细胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并诱导PDC凋亡。

  • AZD1480

    AZD1480是一种新型，ATP竞争性的JAK2抑制剂，无细胞试验中IC50为0.26 nM，选择性作用于JAK3和Tyk2，对JAK1的作用较弱。Phase 1。

    Features:AZD1480为治疗多发性骨髓瘤的潜在新型治疗剂。

  • Fedratinib (TG101348)

    Fedratinib (SAR302503, TG101348)是一种选择性JAK2抑制剂，在无细胞试验中IC50为3 nM，作用于JAK2比作用于JAK1和JAK3选择性高35和334倍。Fedratinib也可抑制 FMS-like tyrosine kinase 3 (FLT3) 和 Ret (c-RET)，对应的IC50值分别为15 nM和48 nM。Fedratinib有潜在的抗肿瘤活性。Fedratinib可抑制细胞增殖并促进凋亡。Phase 2。

  • Momelotinib (CYT387)

    Momelotinib (CYT387, LM-1149 , CYT11387) 是一种ATP竞争性JAK1/JAK2抑制剂，IC50为11 nM/18 nM，比作用于JAK3选择性约高10倍左右。Momelotinib (CYT387) 可诱导凋亡和自噬。Phase 3。

    Features:CYT387是ATP竞争性小分子JAK1 和JAK2抑制剂。

  • WP1066

    WP1066 是一种新型JAK2和STAT3抑制剂，在HEL细胞中IC50分别为2.30 μM和2.43 μM；对JAK2，STAT3，STAT5和ERK1/2具有抑制活性，而对JAK1和JAK3没有作用。WP1066 可诱导凋亡。Phase 1。

    Features:WP1066像它的母体化合物一样能抑制JAK2的磷酸化作用，但与AG490不同WP1066还能减少JAK2的蛋白量。

  • Baricitinib (INCB028050)

    Baricitinib (LY3009104, INCB028050)是一种选择性JAK1和JAK2抑制剂，无细胞试验中IC50分别为5.9 nM和5.7 nM，比作用于JAK3和Tyk2选择性高70和10倍左右，对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞，并用于COVID-19的治疗研究中。Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID