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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
10mM (1mL in DMSO)	RMB 1703.45	现货
5mg	RMB 1317.79	现货
25mg	RMB 2633.61	现货
100mg	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

生物活性

产品描述

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=

Click to View More Cell Line Experimental Data

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]

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

参考文献	[1] Quintas-Cardama A, et al. Blood, 2010, 115(15), 3109-3117. [2] Verstovsek S, et al. N Engl J Med, 2012, 366(9), 799-807. [3] Harrison C, et al. N Engl J Med, 2012, 366(9), 787-798.

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 点击购买： PEG300	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
储存条件	2年	-80°C	溶于溶剂

Download Ruxolitinib (INCB018424) SDF

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 μL 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

%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，注：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：取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：取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
=	×	×

稀释计算器分子量计算器

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)

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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.

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