Ruxolitinib (INCB018424)

目录号:S1378 中文名称:鲁索替尼

仅限科研使用

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。

Ruxolitinib (INCB018424) Chemical Structure

CAS: 941678-49-5

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
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ruxolitinib (INCB018424)发表文献466篇:

产品安全说明书

JAK抑制剂选择性比较

相关JAK产品

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 MlfySpVv[3Srb36gRZN{[Xl? NYnGXGZSPTBizszN MW[yOEBp NWjxbHFnTE2VTx?= NVe2eWNyUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NF\SWo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
SNU182 MWjGeY5kfGmxbjDBd5NigQ>? MnTJOVAh|ryP NHLhfmUzPCCq NEHuPGtFVVOR M2jZ[2lvcGmkaYTpc44hd2ZiU2TBWFEh[W6mIGPURXQ{KHCqb4PwbI9zgWyjdHnvckB{cWewaX\pZ4FvfGy7 MoG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
HuH7 NV7YSZJyTnWwY4Tpc44hSXO|YYm= NHrtOIg2OCEQvF2= MoLHNlQhcA>? Ml;JSG1UVw>? MlTMTY5pcWKrdHnvckBw\iCVVFHUNUBidmRiU2TBWFMheGixc4Doc5J6dGG2aX;uJJNq\26rZnnjZY51dHl? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl2MUizNkc,OjN7NEG4N|I9N2F-
SNU423 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXuUoI2OCEQvF2= NWDafldGPDhiaB?= NHfse5VFVVOR M1jMbF45OSVicnXkeYN1cW:w MnzZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
SNU182 NXnP[FF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi1NEDPxE1? NVO1[lluPDhiaB?= MYPEUXNQ MUW+OlQmKHKnZIXjeIlwdg>? MoLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7NEG4N|IoRjJ|OUSxPFMzRC:jPh?=
HuH7 NH;FWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\OZlUxKM7:TR?= M{X5d|Q5KGh? MWnEUXNQ NUjORopwRjh{JTDy[YR2[3Srb36= NGHRcY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0NVg{Oid-MkO5OFE5OzJ:L3G+
RKO NHvDVFJCeG:ydH;zbZMhSXO|YYm= NILpPIczPSEQvF2= MX60PEBp NE[z[ppFVVOR M{j3e2lv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| MoHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUC1OVAoRjJ2MEWwOVUxRC:jPh?=
DLD-1 MlHkRZBweHSxc3nzJGF{e2G7 Ml;UNlUh|ryP MWi0PEBp Ml6xSG1UVw>? M2XVWmlv\HWlZYOgZZBweHSxc3nzJIJ6KGGldHn2ZZRqdmdiY3HzdIF{\SB| M{\2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvZXmRFPTBizszN NIjQO5o1QCCq NYWwSlhlTE2VTx?= NF\hcmdKSzVyPUG1MlUyKM7:TR?= M1fqUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
RKO MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrNT|c2OCEQvF2= M4H5UFQ5KGh? NE\1OJRFVVOR NEn2[XRKSzVyPUG0Mlc3KM7:TR?= NXrMT4N2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO MkXYT4lv[XOnIFHzd4F6 NF\jW20zPSEQvF2= M17xclQ5KGh? MUfEUXNQ MV;kc4V{KG6xdDDpcohq[mm2IFrBT|EheGixc4Doc5J6dGG2aX;u MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB3MEW1NEc,OjRyNUC1OVA9N2F-
DLD-1 NIrNd|FMcW6jc3WgRZN{[Xl? NYLEO3ZLOjVizszN MXi0PEBp MlT4SG1UVw>? MkPCTY5pcWKrdHnvckBw\iCMQVuyJJBpd3OyaH;yfYxifGmxbh?= NYLjVZN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVA2PTBpPkK0NFUxPTVyPD;hQi=>
RKO NG\mVGFMcW6jc3WgRZN{[Xl? M3\sRlI2KM7:TR?= MUK0PEBp MojiSG1UVw>? MnTETY5pcWKrdHnvckBw\iCMQVuxJJBpd3OyaH;yfYxifGmxbh?= M2\ufFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
DLD-1 MYPLbY5ie2ViQYPzZZk> NEXwWpMzPSEQvF2= NGHXUGs1QCCq NFXyNYZFVVOR M{fhb2lvcGmkaYTpc44hd2ZiSlHLNUBxcG:|cHjvdplt[XSrb36= M4LqZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEWwOVUxLz5{NEC1NFU2ODxxYU6=
BaF3 MV3LbY5ie2ViQYPzZZk> M2DoOlgxKG6P NH3WRnY3KGh? NEjFZ5dFVVOR M2jPfnJm\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\sLiU2TBWFUhcW5iSlHLNnY3OTeILX31eIF1\WRiQlHGN{1GWE:UIHPlcIw> NFjBd3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKzO|c6OSd-MkSyN|c4QTF:L3G+
Huh7 MXLGeY5kfGmxbjDBd5NigQ>? NGjie4IyKM7:TR?= M3rsN|E3KGh? NV;GPZBLTE2VTx?= Mn;1TY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKHOrZ37hcEB1dyCVVFHUNy=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDVyMU[4PUc,OjR3MEG2PFk9N2F-
HepG2 MUfGeY5kfGmxbjDBd5NigQ>? NYn6clIxOSEQvF2= NVXZeZJ3OTZiaB?= MljISG1UVw>? NEDlZ|BKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9ic3nncoFtKHSxIGPURXQ{ M{fYNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUCxOlg6Lz5{NEWwNVY5QTxxYU6=
Hep3B M1\mOGZ2dmO2aX;uJGF{e2G7 NW\ic|NyOSEQvF2= NX7B[GRROTZiaB?= MV\EUXNQ MkjaTY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKGGldHn2[UBUXEGWMzD3bZRpKEmFNUCgc4YhhjVyIN88US=> NFTXVIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEWwNVY5QSd-MkS1NFE3QDl:L3G+
NCI-H2347 MlXERZBweHSxc3nzJGF{e2G7 NXT2e5E5OzBibl2= MlHzOFghcA>? M3jrcGROW09? MmrYTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 M4n2T2Fxd3C2b4Ppd{BCe3OjeR?= M2rvblMxKG6P NXu1SJlkPDhiaB?= NVmzOYxxTE2VTx?= M2np[mlv\HWldHnvckBw\iCjcH;weI9{cXN? M{DzWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkGzOlcxLz5{NUKxN|Y4ODxxYU6=
A549/DDP NWXldVFHSXCxcITvd4l{KEG|c3H5 MmH1N|Ahdk1? M1vrXlQ5KGh? MUXEUXNQ NFfSe|hKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJzM{[3NEc,OjV{MUO2O|A9N2F-
NCI-H1299 NHvGW5RHfW6ldHnvckBCe3OjeR?= M4Xv[FMxKG6P M37TeFQ5KGh? NG\2SZhFVVOR MYXEc5dvNXKnZ4XsZZRqd25ib3[gV3RCXDNicHjvd5Bpd3K7bHH0bY9v NU\Qd4lZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
NCI-H2347 NGHIeJRHfW6ldHnvckBCe3OjeR?= NFHDNpQ{OCCwTR?= M1T6TlQ5KGh? NV3aWGxZTE2VTx?= MUHE[YNz\WG|ZTDpckBD[2x{IHX4dJJme3Orb36= NY\UeGFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNVM3PzBpPkK1NlE{PjdyPD;hQi=>
A549/DDP M1Hnb2Z2dmO2aX;uJGF{e2G7 MUWzNEBvVQ>? NXjKUIc5PDhiaB?= M3;mUWROW09? M4rnVmRwf25vcnXneYxifGmxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25? Ml3LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
NCI-H2347 NVjCbmFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPEUXNQ NGrTeY5KSzVyPUCuNVch|ryP NGHC[ms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H1299 M2i5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzsNZdFVVOR M3PPWmlEPTB;MD6yPEDPxE1? Mn3XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MUO2O|AoRjJ3MkGzOlcxRC:jPh?=
A549/DDP M1ns[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP3fXQ2TE2VTx?= M4\iUGlEPTB;MD6yNkDPxE1? NITSNWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
A549 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorLSG1UVw>? NFHYR45KSzVyPUCuNFQh|ryP NET5VI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H358 MnfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHCbmVFVVOR NVLYdnhrUUN3ME2wMlEh|ryP NEHzdmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
NCI-H460 NWLvU4ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXMSG1UVw>? NHzxbFRKSzVyPUCuNVMh|ryP NF;PXWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKxN|Y4OCd-MkWyNVM3PzB:L3G+
CMK M1HkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\nUJN4UW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MkGyOEc,OjV|NUKxNlQ9N2F-
CMK NHGxN2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fUbmlvcGmkaYTpc44hd2ZiQ13LJINienK7aX7nJJRp\SCMQVuzRVY{TCCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTZ|IN88US=> M1LveVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{WyNVI1Lz5{NUO1NlEzPDxxYU6=
CMK MkTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonBTY5pcWKrdHnvckBw\iCFTVugZ4FzenmrbnegeIhmKEqDS{PBOVczXiCvdYTheIlwdiClZXzsJJBzd2yrZnXyZZRqd25? NF;qfWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO1NlEzPCd-MkWzOVIyOjR:L3G+
HT93A MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETGXIU{OjBibl2= NWPvXIZYPSCm NG\Q[3lFVVOR NWj1OVJVUW6qaXLpeIlwdiCxZjDHR3MuTiCrbnT1Z4VlKGe{YX71cI9kgXSrYzDkbYZn\XKnboTpZZRqd25? NGG4eYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUiwOVk3Oid-MkW4NFU6PjJ:L3G+
SET-2 M4TyWmN6fG:2b4jpZ{BCe3OjeR?= M2ft[lUh|ryP MnjDOFghcA>? NH;RV5FEgXSxdH;4bYMhcW6mZYi9NVgvPyV? M{TrUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUOxN|Q6Lz5{NUmzNVM1QTxxYU6=
HEL MoruR5l1d3SxeHnjJGF{e2G7 MkPqOUDPxE1? MVO0PEBp MVTDfZRwfG:6aXOgbY5l\Xh;MUKuNkU> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl|MUO0PUc,OjV7M{GzOFk9N2F-
Human monocyte NHvRNGlMcW6jc3WgRZN{[Xl? NIPmdJBKdmirYnn0bY9vKG:oIFrBT|IwOSCrbjDoeY1idiCvb37vZ5l1\XNiZYjwdoV{e2mwZzDDSFE1KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUU[QZ3HtcYEue3SrbYXsZZRm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEOx{txO MkLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
Human monocyte M3L5SGtqdmG|ZTDBd5NigQ>? Mle1TY5pcWKrdHnvckBw\iCMQVuyJIlvKGi3bXHuJI1wdm:leYTld{BmgHC{ZYPzbY5oKEOGMUSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDHUU1EW0Zvc4TpcZVt[XSnZDDTWGFVPWFicHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAzPs7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2ME[0PEc,OjN3NEC2OFg9N2F-
Human T cell NGLYWZlMcW6jc3WgRZN{[Xl? M2rHWWlvcGmkaYTpc44hd2ZiSlHLN{8yKGmwIHj1cYFvKFRiY3XscJMh\XiycnXzd4lv\yCFREOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUFIue3SrbYXsZZRm\CCVVFHUOYEheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyN:69VQ>? MojEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC2OFgoRjJ|NUSwOlQ5RC:jPh?=
TF1 M2K3fGtqdmG|ZTDBd5NigQ>? NVf5VoZFOjBibXnu MnXsSG1UVw>? MnXKTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNPi2rbnT1Z4VlKFOWQWSzJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkVOwG0> MkfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
TF1 MmPGT4lv[XOnIFHzd4F6 MkDtNlAhdWmw M3nsWmROW09? M1LwTGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBGWE9vaX7keYNm\CCVVFHUOUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEGy{txO NFLCfVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[5PFA5PCd-MkK2PVgxQDR:L3G+
Sf9 cells MlnjTmFMKGmwaHnibZRqd25iYYPzZZk> Ml\BNUBp NX\SZld2U2liPTCwMlAxODFizszN M3nhO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf9 cells NXrDNIMxUkGNIHnubIljcXSrb36gZZN{[Xl? MoGxNUBp NWfVZ2ttU2liPTCwMlAxODJizszN MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
Sf9 cells MYPKRWshcW6qaXLpeIlwdiCjc4PhfS=> NEjvOZIyKGh? MlPST4khRSByLkCwNFUh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4OES4OEc,OjN4Nki0PFQ9N2F-
SET2 cells MmrZTmFMKGmwaHnibZRqd25iYYPzZZk> NHj2d|NKSzVyIE2gNE4xODF6NDFOwG0> NXm0WZl1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOlE3PjBpPkKzNFYyPjZyPD;hQi=>
Sf21 cells NFTUWWNLSUtiaX7obYJqfGmxbjDhd5NigQ>? M{npb|EhcA>? NEPjNYFKSzVyIE2gNE4xODJ6IN88US=> M1\4Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUmxOFAzLz5{MkW5NVQxOjxxYU6=
Sf21 cells Mm\QTmFMKGmwaHnibZRqd25iYYPzZZk> MnPIOlAhdWmw M3v1bWlEPTBiPTCwMlAxOyEQvF2= M134dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUO3N|U6Lz5{N{GzO|M2QTxxYU6=
Sf9 cells NGjTcGNLSUtiaX7obYJqfGmxbjDhd5NigQ>? M4LxVFEhcA>? Mn7BT4khRSByLkCwN|Ih|ryP M13jRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[4OFg1Lz5{M{[2PFQ5PDxxYU6=
Sf21 cells MUHKRWshcW6qaXLpeIlwdiCjc4PhfS=> NVTacFU1OSCq MYPJR|UxKD1iMD6wNFM{KM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV7MUSwNkc,OjJ3OUG0NFI9N2F-
TF1 cells NFOzR5VLSUtiaX7obYJqfGmxbjDhd5NigQ>? MYKzNEBucW5? MYPJR|UxKD1iMD6wNFY5PSEQvF2= MoPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkG2OlAoRjJ|ME[xOlYxRC:jPh?=
CD34+ cells Mm\BTmFMKGmwaHnibZRqd25iYYPzZZk> MnPITWM2OCB;IECuNFA5KM7:TR?= NXfDTJlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5Nlc1OjNpPkK2PVI4PDJ|PD;hQi=>
TF1 cells MVHKRWshcW6qaXLpeIlwdiCjc4PhfS=> M3i5SVIxKG2rbh?= NITCS41GSzVyIE2gNE4xOTJizszN MlzSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
Sf21 cells Ml;VWHlMOiCrbnjpZol1cW:wIHHzd4F6 MXexJIg> NYHCUZk3UUN3MDC9JFAvODF7IN88US=> Ml;TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3OUG0NFIoRjJ{NUmxOFAzRC:jPh?=
T cells NGC0NVVLSUtiaX7obYJqfGmxbjDhd5NigQ>? M2CxRmlEPTBiPTCwMlAzOyEQvF2= M4WyfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwOlQ5Lz5{M{W0NFY1QDxxYU6=
T cells MkPRTmFMKGmwaHnibZRqd25iYYPzZZk> MonmTWM2OCB;IECuNFI{KM7:TR?= NGq2d3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFY1QCd-MkO1OFA3PDh:L3G+
TF1 cells M4KxeGpCUyCrbnjpZol1cW:wIHHzd4F6 NIntXZczOCCvaX6= NEHGPWdGSzVyIE2gNE4xOjRizszN MoPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4OUiwPFQoRjJ{Nkm4NFg1RC:jPh?=
T cells NUDGd4tiUkGNIHnubIljcXSrb36gZZN{[Xl? MU\JR|UxKD1iMD6wN|Eh|ryP NUfuc4xWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
T cells MYTKRWshcW6qaXLpeIlwdiCjc4PhfS=> MWjJR|UxKD1iMD6wN|Eh|ryP NYHS[FluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA3PDhpPkKzOVQxPjR6PD;hQi=>
PBMC cells NVXoem57UkGNIHnubIljcXSrb36gZZN{[Xl? NVK0VoJIUUN3MDC9JFAvODRizszN MlSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7Mke0NlMoRjJ4OUK3OFI{RC:jPh?=
Sf21 cells NW\nSFhOUkGNIHnubIljcXSrb36gZZN{[Xl? NWH3O2FoOSCq MnnTTWM2OCB;IECuOFI5KM7:TR?= NEfvcnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW5NVQxOid-MkK1PVE1ODJ:L3G+
PBMC cells MkjHV3RCXDViaX7obYJqfGmxbjDhd5NigQ>? NWPmNlE4UUN3MDC9JFAvPDR6IN88US=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl{N{SyN{c,OjZ7Mke0NlM9N2F-
CD34+ cells M2i5dWpCUyCrbnjpZol1cW:wIHHzd4F6 M3\FOlQ2KG2rbh?= NXfMdllPUUN3MDC9JFAvPjd5IN88US=> M3znbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVM{Lz5{NESxO|U{OzxxYU6=
Assay
Methods Test Index PMID
Western blot cleaved PARP / cleaved caspase3 p-JAK2 / p-AKT / p-MAPK / Bcl-xl / MCL-1 c-Myc / c-Jun / Cyclin B / Cyclin D / Bcl-2 / HIF-1α p-STAT3 29849942 30930994
Growth inhibition assay Cell viability Cell apoptosis Cell proliferation 29849942 29515770
Immunofluorescence α-tubulin 26356819
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]
  • 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]
  • 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。
动物实验:[1]
  • Animal Models: JAK2V617F驱动的小鼠模型
  • Dosages: 180 mg/kg
  • Administration: 口服

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05280509 Not yet recruiting Drug: TL-895|Drug: Ruxolitinib Myelofibrosis|Primary Myelofibrosis|Post-PV MF|Post-ET Myelofibrosis Telios Pharma Inc. October 2022 Phase 1|Phase 2
NCT05456529 Not yet recruiting Drug: Ruxolitinib Cream Atopic Dermatitis (AD) Incyte Corporation August 19 2022 Phase 3
NCT05247489 Recruiting Drug: Ruxolitinib 1.5% cream|Device: NB-UVB phototherapy Vitiligo|JAK Inhibitor Incyte Corporation May 5 2022 Phase 2
NCT05371964 Recruiting Drug: Imetelstat|Drug: Ruxolitinib Myelofibrosis Geron Corporation May 4 2022 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们

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.

Tags: buy Ruxolitinib (INCB018424) | Ruxolitinib (INCB018424) supplier | purchase Ruxolitinib (INCB018424) | Ruxolitinib (INCB018424) cost | Ruxolitinib (INCB018424) manufacturer | order Ruxolitinib (INCB018424) | Ruxolitinib (INCB018424) distributor