Ruxolitinib (INCB018424)

目录号:S1378

Ruxolitinib (INCB018424) Chemical Structure

Molecular Weight(MW): 306.37

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。

规格 价格 库存 购买数量  
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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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。
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
TF1 NFrpe|NMcW6jc3WgRZN{[Xl? NWD4V4hGOjBibXnu NUXSUWI6TE2VTx?= NFH0d4FKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXEZzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVCRLXnu[JVk\WRiU2TBWFUheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCxNu69VQ>? Ml;CNlI3QThyOES=
TF1 MVvLbY5ie2ViQYPzZZk> MliyNlAhdWmw Mk\XSG1UVw>? M1KyeWlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBKVDZvaX7keYNm\CCVVFHUN{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEK0{txO MYKyNlY6QDB6NB?=
Human T cell NFOzSoFMcW6jc3WgRZN{[Xl? MmPrTY5pcWKrdHnvckBw\iCMQVuzM|EhcW5iaIXtZY4hXCClZXzsd{BmgHC{ZYPzbY5oKEOGMzDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMNk1{fGmvdXzheIVlKFOWQWS1ZUBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKz{txO M4\CWVI{PTRyNkS4
Human monocyte M4TPdWtqdmG|ZTDBd5NigQ>? NWXoellsUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKG2xbn;jfZRmeyCneIDy[ZN{cW6pIFPENVQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBIVS2FU1[td5RqdXWuYYTl[EBUXEGWNXGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjB{Nt88US=> MmThNlM2PDB4NEi=
Human monocyte M1vCbmtqdmG|ZTDBd5NigQ>? MVXJcohq[mm2aX;uJI9nKEqDS{KvNUBqdiCqdX3hckBud26xY4n0[ZMh\XiycnXzd4lv\yCFREG0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWZP\2GvbXGtd5RqdXWuYYTl[EBUXEGWMTDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODNzzszN MWWyN|U1ODZ2OB?=
HEL NH;pOIlEgXSxdH;4bYMhSXO|YYm= MkKxOUDPxE1? MlP3OFghcA>? MkToR5l1d3SxeHnjJIlv\GW6PUGyMlIm MXKyOVk{OTN2OR?=
SET-2 MXfDfZRwfG:6aXOgRZN{[Xl? M2PJdFUh|ryP NXH5SY53PDhiaB?= M{HMVGN6fG:2b4jpZ{BqdmSneE2xPE44LQ>? MXiyOVk{OTN2OR?=
HT93A MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnvdHA2OzJyIH7N NWfEcXdYPSCm MlO5SG1UVw>? MorNTY5pcWKrdHnvckBw\iCJQ2OtSkBqdmS3Y3XkJIdz[W63bH;jfZRq[yCmaX\m[ZJmdnSrYYTpc44> NX3B[4dFOjV6MEW5OlI>
CMK MmTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzwNJhwUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPTd{VjDteZRifGmxbjDj[YxtKHC{b3zp[oVz[XSrb36= NIrTZZQzPTN3MkGyOC=>
CMK MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHpZ5RZUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIFrBT|NCPjOGIH31eIF1cW:wIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zNkOg{txO NY\MUGxTOjV|NUKxNlQ>
CMK NXfKbVg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULN[FdrUW6qaXLpeIlwdiCxZjDDUWsh[2G{conpcochfGinIGfUJGpCUyClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvODd3IN88US=> MYmyOVM2OjF{NB?=
NCI-H460 NFHqS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPZdFBFVVOR NXTSbYxDUUN3ME2wMlE{KM7:TR?= NVS0dIIyOjV{MUO2O|A>
NCI-H358 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfEUXNQ NHXJOI9KSzVyPUCuNUDPxE1? NV76[XliOjV{MUO2O|A>
A549 NXL0cmI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;EUXNQ NFr4XmZKSzVyPUCuNFQh|ryP MUCyOVIyOzZ5MB?=
A549/DDP NGPu[2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPPT2FRTE2VTx?= NV3ZPFFLUUN3ME2wMlIzKM7:TR?= MVKyOVIyOzZ5MB?=
NCI-H1299 NYnPNmNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jpZ2ROW09? NVzsUG92UUN3ME2wMlI5KM7:TR?= MVuyOVIyOzZ5MB?=
NCI-H2347 NGHGWI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDlSG1UVw>? NXX0eGp5UUN3ME2wMlE4KM7:TR?= M4jtR|I2OjF|Nkew
A549/DDP M4SwPGZ2dmO2aX;uJGF{e2G7 Mlz5N|Ahdk1? M13xWFQ5KGh? NYnUbI4zTE2VTx?= NX21eJNLTG:5bj3y[Yd2dGG2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbh?= MV:yOVIyOzZ5MB?=
NCI-H1299 MVvGeY5kfGmxbjDBd5NigQ>? MY[zNEBvVQ>? M4nieFQ5KGh? Mk\lSG1UVw>? Mm\2SI94di2{ZXf1cIF1cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? MUOyOVIyOzZ5MB?=
NCI-H2347 NV7mWoQ2TnWwY4Tpc44hSXO|YYm= NFy0eVY{OCCwTR?= NHrTd4I1QCCq NIXEe|JFVVOR NHy3NlZF\WO{ZXHz[UBqdiCEY3yyJIV5eHKnc4Ppc44> MVeyOVIyOzZ5MB?=
A549/DDP M1\jU2Fxd3C2b4Ppd{BCe3OjeR?= NFrpTlE{OCCwTR?= M1f0[FQ5KGh? NUfYWWROTE2VTx?= MXTJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NXiyRWZwOjV{MUO2O|A>
NCI-H1299 M{K5cGFxd3C2b4Ppd{BCe3OjeR?= NXH6N|hmOzBibl2= MXq0PEBp NF3nfIRFVVOR NHnDSpRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NVLOU3NIOjV{MUO2O|A>
NCI-H2347 NVuyU3I5SXCxcITvd4l{KEG|c3H5 NWTSeFNYOzBibl2= M36zdlQ5KGh? MnzqSG1UVw>? NGizepJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M1\vOVI2OjF|Nkew
Hep3B MnTUSpVv[3Srb36gRZN{[Xl? NULseFJOOSEQvF2= NETBVXUyPiCq MVfEUXNQ NHixPZdKdXCjaYLld{B1cGViY3HwZYNqfHlib3[gTWhESS2jc4PvZ4lifGWmIHfwNVMxKG23dHHueJMhfG9iYXP0bZZmKFOWQWSzJJdqfGhiSVO1NEBw\iC-NUCg{txO NVywTVdlOjR3MEG2PFk>
HepG2 NETycnlHfW6ldHnvckBCe3OjeR?= M1j5O|Eh|ryP NXzNNWdpOTZiaB?= M320UGROW09? MU\JcZBicXKnczD0bIUh[2GyYXPpeJkhd2ZiSVjDRU1ie3OxY3nheIVlKGeyMUOwJI12fGGwdIOgeI8he2mpbnHsJJRwKFOWQWSz NYTse4ZyOjR3MEG2PFk>
Huh7 MnznSpVv[3Srb36gRZN{[Xl? NU\VdG1EOSEQvF2= NET5ZYIyPiCq NITjRohFVVOR MkXwTY1x[Wm{ZYOgeIhmKGOjcHHjbZR6KG:oIFnIR2Eu[XO|b3PpZZRm\CCpcEGzNEBufXSjboTzJJRwKHOrZ37hcEB1dyCVVFHUNy=> MUmyOFUxOTZ6OR?=
BaF3 MoXUT4lv[XOnIFHzd4F6 M4H2PFgxKG6P M{HhfFYhcA>? MmXJSG1UVw>? NES2TG1T\WS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hd2cEoGPURXQ2KGmwIFrBT|JXPjF5Rj3teZRifGWmIFLBSlMuTVCRUjDj[Yxt NUnxUYVOOjR{M{e3PVE>
DLD-1 NVP3bGhKU2mwYYPlJGF{e2G7 NG\MbYkzPSEQvF2= MXq0PEBp MWfEUXNQ MY\Jcohq[mm2aX;uJI9nKEqDS{GgdIhwe3Cqb4L5cIF1cW:w Mmm0NlQxPTB3NUC=
RKO NWDQfIJWU2mwYYPlJGF{e2G7 NYjaXGo{OjVizszN NVvpVnFEPDhiaB?= MV7EUXNQ NWrOeXpHUW6qaXLpeIlwdiCxZjDKRWsyKHCqb4PwbI9zgWyjdHnvci=> MmS0NlQxPTB3NUC=
DLD-1 NESwU4dMcW6jc3WgRZN{[Xl? NF\UR20zPSEQvF2= MXO0PEBp MW\EUXNQ MYDJcohq[mm2aX;uJI9nKEqDS{KgdIhwe3Cqb4L5cIF1cW:w MX:yOFA2ODV3MB?=
RKO NWPJZnBCU2mwYYPlJGF{e2G7 NWm2RnJsOjVizszN M4L5SFQ5KGh? NV7Bd29ITE2VTx?= NED3fJNld2W|IH7veEBqdmirYnn0JGpCUzFicHjvd5Bpd3K7bHH0bY9v Mnj4NlQxPTB3NUC=
DLD-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPZNYh3PTBizszN NVfiXYxjPDhiaB?= MV3EUXNQ NUHlfIl3UUN3ME2xOU42OSEQvF2= MV[yOFA2ODV3MB?=
RKO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWi1NEDPxE1? MlftOFghcA>? Moi1SG1UVw>? NHW1Ro9KSzVyPUG0Mlc3KM7:TR?= NFHZb|EzPDB3MEW1NC=>
DLD-1 M2G3VGFxd3C2b4Ppd{BCe3OjeR?= NFzEclkzPSEQvF2= MUC0PEBp MWPEUXNQ MmnnTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? MXOyOFA2ODV3MB?=
RKO MV7BdI9xfG:|aYOgRZN{[Xl? M4rs[VI2KM7:TR?= MkPaOFghcA>? M1XJN2ROW09? MnfqTY5lfWOnczDhdI9xfG:|aYOgZpkh[WO2aY\heIlv\yClYYPwZZNmKDN? M4XhXlI1ODVyNUWw
HuH7 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHqfIo2OCEQvF2= MYG0PEBp MX;EUXNQ MXq+PFImKHKnZIXjeIlwdg>? MWWyN|k1OTh|Mh?=
SNU182 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInRcW82OCEQvF2= M1jI[lQ5KGh? MWnEUXNQ MlnsQlY1LSC{ZXT1Z5Rqd25? NV65d5hJOjN7NEG4N|I>
SNU423 NG\iR5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;FOVAh|ryP M4Tkb|Q5KGh? MXTEUXNQ Mnm3QlgyLSC{ZXT1Z5Rqd25? MlLLNlM6PDF6M{K=
HuH7 MnzvSpVv[3Srb36gRZN{[Xl? M4CxfVUxKM7:TR?= M1vNU|I1KGh? NEfYWWZFVVOR NV3zfGRiUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NWW0So9{OjN7NEG4N|I>
SNU182 NYXQeJNnTnWwY4Tpc44hSXO|YYm= NG\UZ5M2OCEQvF2= NVn3eIYzOjRiaB?= NX\iUFZJTE2VTx?= NULJRZZmUW6qaXLpeIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKHOrZ37p[olk[W62bIm= NF2wTJYzOzl2MUizNi=>
SNU423 NVrJUoFJTnWwY4Tpc44hSXO|YYm= NXPmSHdzPTBizszN M3;PSVI1KGh? M{fXRmROW09? MUXJcohq[mm2aX;uJI9nKFOWQWSxJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36gd4lodmmoaXPhcpRtgQ>? MUiyN|k1OTh|Mh?=

... 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]
+ 展开

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]
+ 展开
  • 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]
+ 展开
  • Animal Models: JAK2V617F驱动的小鼠模型
  • Formulation: 5%二甲基乙酰胺,0.5%methocellulose
  • 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 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03571321 Not yet recruiting Acute Lymphoblastic Leukemia|ALL Childhood|ALL University of Chicago|Incyte Corporation September 5 2019 Phase 1
NCT03571321 Not yet recruiting Acute Lymphoblastic Leukemia|ALL Childhood|ALL University of Chicago|Incyte Corporation September 5 2019 Phase 1
NCT03801434 Not yet recruiting BCR-JAK2 Fusion Protein Expression|Blasts 20 Percent or Less of Peripheral Blood White Cells|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells|Blasts More Than 5 Percent of Peripheral Blood White Cells|Blasts Under 20 Percent of Bone Marrow Nucleated Cells|Chronic Eosinophilic Leukemia Not Otherwise Specified|Eosinophilia|Hepatomegaly|Hypereosinophilic Syndrome|JAK2 Gene Mutation|Splenomegaly|TEL-JAK2 Fusion Protein Expression Stanford University|Incyte Corporation June 19 2019 Phase 2
NCT03801434 Not yet recruiting BCR-JAK2 Fusion Protein Expression|Blasts 20 Percent or Less of Peripheral Blood White Cells|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells|Blasts More Than 5 Percent of Peripheral Blood White Cells|Blasts Under 20 Percent of Bone Marrow Nucleated Cells|Chronic Eosinophilic Leukemia Not Otherwise Specified|Eosinophilia|Hepatomegaly|Hypereosinophilic Syndrome|JAK2 Gene Mutation|Splenomegaly|TEL-JAK2 Fusion Protein Expression Stanford University|Incyte Corporation June 19 2019 Phase 2
NCT03610971 Not yet recruiting Chronic Phase Chronic Myeloid Leukemia|Chronic Myeloid Leukemia Chronic Phase H. Lee Moffitt Cancer Center and Research Institute|H. Jean Khoury Cure CML Consortium|Incyte Corporation May 2019 Phase 2
NCT03722407 Not yet recruiting Chronic Myelomonocytic Leukemia|Leukemia H. Lee Moffitt Cancer Center and Research Institute|Incyte Corporation May 1 2019 Phase 2

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操作手册

如果有其他问题,请给我们留言。

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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.

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